Books
Silverman, R.B. Mechanism-Based Enzyme Inactivation: Chemistry and Enzymology, Vols. I and II; CRC Press: Boca Raton, FL; 1988.
2a. Silverman, R.B. The Organic Chemistry of Drug Design and Drug Action; Academic Press: San Diego; 1992.
2b. Silverman, R. B. Medizinische Chemie für Organiker, Biochemiker und Pharmazeutische Chemiker, VCH: Weinheim; 1995 (German Translation by Joachim K. Seydel of The Organic Chemistry of Drug Design and Drug Action).
3. Silverman, R. B. The Organic Chemistry of Enzyme-Catalyzed Reactions, Academic Press: San Diego; 2000; revised, 2002.
4. Silverman, R.B. The Organic Chemistry of Drug Design and Drug Action; 2nd Edition; Elsevier/Academic Press: San Diego; 2004.
5. Silverman, R.B.; Holladay, M. W. The Organic Chemistry of Drug Design and Drug Action; 3rd Edition; Elsevier/Academic Press: San Diego; 2014.
Articles
1. Silverman, R.B.; Olofson, R.A. Chem. Commun., 1968, 1313. “The Oxidation of Tungsten Carbonyl in Carbon Tetrachloride.”
2. Klayman, D.L.; Kenny, D.; Silverman, R.B.; Tomaszewski, J.E.; Shine, R.J. J. Org. Chem., 1971, 36, 3681-3686. “The Action of Hydrogen Sulfide on Aminoalkanethiosulfuric Acids (Bunte Salts) to Give Di-, Tri-, and Tetrasulfides.”
3. Silverman, R.B.; Dolphin, D.; Babior, B.M. J. Am. Chem. Soc., 1972, 94, 4028-4030. “A Model for the Mechanism of Action of Coenzyme B12 Dependent Enzymes. Evidence for σÆ π Rearrangements in Cobaloximes.”
4. Silverman, R.B.; Dolphin, D. J. Am. Chem. Soc., 1973, 95, 1686-1688. “A Direct Method for Cobalt-Carbon Bond Formation in Cobalt (III)-Containing Cobalamins and Cobaloximes. Further Support for Cobalt(III) π Complexes in Coenzyme B12 Dependent Rearrangements.”
5. Silverman, R.B. in Klayman, D.L.; Gunther, W.H.H. Organic Selenium Compounds: Their Chemistry and Biology, Chapter VII, Wiley-Interscience, New York, 1973. “Selenium Analogs of Aldehydes and Ketones.”
6. Silverman, R.B. in Klayman, D.L.; Gunther, W.H.H. Organic Selenium Compounds: Their Chemistry and Biology, Chapter XI, Wiley-Interscience, New York, 1973. “Miscellaneous Selenium-Containing Heterocycles.”
7. Silverman, R.B.; Dolphin, D. J. Am. Chem. Soc., 1974, 96, 7094-7096. “Reactions of Vinyl Ethers with Cobaloximes and Cobalamins.”
8. Silverman, R.B.; Dolphin, D.; Carty, T.J.; Krodel, E.K.; Abeles, R.H. J. Am. Chem. Soc., 1974, 96, 7096-7097. “Formylcobalamin.”
9. Silverman, R.B.; Dolphin, D. J. Am. Chem. Soc., 1975, 97, 2924-2925. “On the Mechanisms of Hydrolysis of β-Acetal Cobalamins.”
10. Silverman, R.B.; Dolphin, D. J. Organometal. Chem., 1975, 101, C14-C16. “Hydrolysis of β-Acetal Cobaloximes.”
11. Silverman, R.B.; Dolphin, D. J. Am. Chem. Soc., 1976, 98, 4626-4633. “Model Studies for Coenzyme B12-Dependent Enzyme-Catalyzed Rearrangements: Evidence for Co(III)-p Complexes.”
12. Silverman, R.B.; Dolphin, D. J. Am. Chem. Soc., 1976, 98, 4633-4639. “Model Studies for Coenzyme B12-Dependent Enzyme-Catalyzed Rearrangements: Kinetics and Mechanism of Decomposition of Formylmethyl-cobalamin and Its Acetals.”
13. Silverman, R.B.; Dolphin, D. Can. J. Chem., 1976, 54, 1425-1427. “Alkylation of the Dimethylglyoximato Ligands in Reduced Cobaloxime.”
14. Silverman, R.B.; Abeles, R.H. Biochemistry, 1976, 15, 4718-4723. “Inactivation of Pyridoxal Phosphate-Dependent Enzymes by Mono- and Polyhaloalanines.”
15. Silverman, R.B.; Abeles, R.H. Biochemistry, 1977, 16, 5515-5520. “Mechanism of Inactivation of γ-Cystathionase by β,β,β-Trifluoroalanine.”
16. Silverman, R.B.; Kapili, L.V. J. Chromatography, 1978, 161, 415-416. “Paper Chromatographic and Electrophoretic Separations of Orotic Acid, 5-Fluoroorotic Acid, 5-Fluorouracil, and 5-Fluorouridine 5′-Monophosphate.”
17. Silverman, R.B. J. Heterocycl. Chem., 1978, 15, 1519-1520. “Reaction of Diethyl Acetonedicarboxylate with Nitrosyl Chloride.”
18. Silverman, R.B.; Kapili, L.V. J. Label. Compounds Radiopharm., 1979, 16, 361-364. “Synthesis of [Carboxyl-14C]5-Fluoroorotic Acid.”
19. Silverman, R.B.; Hoffman, S.J. in Kalman, T.I. (Edit.) Drug Action and Design: Mechanism-Based Enzyme Inhibitors, Elsevier-North Holland, N.Y., 1979, pp 175-186, “Mechanism of Inactivation of Mitochondrial Monoamine Oxidase by Cyclopropylamines.”
20. Silverman, R.B.; Hoffman, S.J. in Singer, T.P.; Von Korff, R.W.; Murphy, D.L. (Edit.) Monoamine Oxidase: Structure, Function, and Altered Functions, Academic Press, N.Y., 1979, pp 71-79, “Mechanism of Inactivation of Monoamine Oxidase by N-Cyclopropyl-N-Arylalkyl Amines.”
21. Silverman, R.B.; Radak, R.E.; Hacker, N.P. J. Org. Chem., 1979, 44, 4970-4971. “A Mild Method of Hydrolysis of 2,4-Dialkoxy-6-Substituted Pyrimidines to 6-Substituted Uracils.”
22. Dolphin, D.; Banks, A.R.; Cullen, W.R.; Cutler, A.R.; Silverman, R.B. in Zagalak, B.; Friedrich, W. (Edit.) Proceedings of the Third European Symposium on Vitamin B12 and Intrinsic Factor, Walter deGruyter, Inc., Berlin and N.Y., 1979. “The Mechanism of Action of Coenzyme B12.”
23. Bulkowski, J.; Cutler, A.; Dolphin, D.; Silverman, R.B. Inorganic Syntheses, 1980, 20, 127-134. “Bis[2,3-butanedionedioximato (1-)]cobalt Complexes.”
24. Dolphin, D.; Halko, D.J.; Silverman, R.B. Inorganic Syntheses, 1980, 20, 134-142. “Cobalamins and Cobinamides.”
25. Silverman, R.B.; Levy, M.A. J. Org. Chem., 1980, 45, 815-818. “Syntheses of (S)-5-Substituted-4-Aminopentanoic Acids: A New Class of γ-Aminobutyric Acid Transaminase Inactivators.”
26. Silverman, R.B.; Hoffman, S.J. J. Am. Chem. Soc., 1980, 102, 884-886. “Mechanism of Inactivation of Mitochondrial Monoamine Oxidase by N-Cyclopropyl-N-Arylalkyl Amines.”
27. Silverman, R.B.; Dolphin, D. J. Chromatography, 1980, 194, 273-274. “Thin-Layer Chromatography of Acid-Labile Cobalamins.”
28. Silverman, R.B. J. Am. Chem. Soc., 1980, 102, 5421-5423. “A Model for a “Molecular Mechanism of Anticoagulant Activity of 3-Substituted-4-Hydroxycoumarins.”>
29. Silverman, R.B.; Levy, M.A. Biochem. Biophys. Res. Comm., 1980, 95, 250-255. “Irreversible Inactivation of Pig Brain γ-Aminobutyric Acid-α-Ketoglutarate Transaminase by 4-Amino-5-halopentanoic Acids.”
30. Silverman, R.B.; Hoffman, S.J.; Catus, W.B., III J. Am. Chem. Soc., 1980, 102, 7126-7128. “A Mechanism for Mitochondrial Monoamine Oxidase-Catalyzed Amine Oxidation.”
31. R.B. Silverman, J. Am. Chem. Soc., 1981, 103, 3910-3915. “Model Studies for a Molecular Mechanism of Action of Oral Anticoagulants.”
32. Silverman, R.B.; Hoffman, S.J. J. Label. Compounds Radiopharm., 1981, 18, 781-790. “Syntheses of N-[1-2H]-, N-[1-3H]cyclopropylbenzylamine and [phenyl-14C]N-cyclopropylbenzylamine.”
33. Silverman, R.B.; Levy, M.A. Biochemistry, 1981, 20, 1197-1203. “Mechanism of Inactivation of γ-Aminobutyric Acid-α-Ketoglutaric Acid Aminotransferase by 4-Amino-5-halopentanoic Acids.”
34. Silverman, R.B.; Levy, M.A. J. Biol. Chem., 1981, 256, 11565-11568. “Substituted 4-Aminobutanoic Acids: Substrates for γ-Aminobutyric Acid-α-Ketoglutaric Acid Aminotransferase.”
35. Silverman, R.B. J. Am. Chem. Soc., 1981, 103, 5939-5941, “Chemical Model Studies for the Mechanism of Vitamin K Epoxide Reductase.”
36. Silverman, R.B. J. Org. Chem., 1981, 46, 4789-4791, “Mechanism of Isomerization of a β-Ketosulfide.”
37. Silverman, R.B.; Hoffman, S.J. Biochem. Biophys. Res. Commun. 1981, 101, 1396-1401. “N-(1-Methyl)Cyclopropylbenzylamine: A Novel Inactivator of Mitochondrial Monoamine Oxidase.”
38. Silverman, R.B.; Levy, M.A.; Muztar, A.J.; Hirsch, J.D. Biochem. Biophys. Res. Commun., 1981, 102, 520-523. “In Vivo Inactivation of γ-Aminobutyric Acid-α-Ketoglutarate Transaminase by 4-Amino-5-fluoropentanoic Acid.”
39. Silverman, R.B.; Holladay, M.W. J. Am. Chem. Soc., 1981, 103, 7357-7358. “Stereospecific Total Syntheses of the Antitumor Agent [αS,5S]-α-Amino-3-chloro-4,5-dihydro-5-isoxazoleacetic Acid and Its C-5 Epimer.”
40. Silverman, R.B.; Hoffman, S.J.; Catus, W.B., III in Flavins and Flavoproteins, (V. Massey and C.H. Williams, Jr., eds.) Elsevier-North Holland, N.Y., 1982, pp. 213-216, “A Mechanism for Mitochondrial Monoamine Oxidase-Catalyzed Amine Oxidation.”
41. Silverman, R.B.; Groziak, M.P. J. Am. Chem. Soc., 1982, 104, 6434-6439. “Model Chemistry for a Covalent Mechanism of Action of Orotidine 5′-Phosphate Decarboxylase.”
42. Silverman, R.B.; Muztar, A.J.; Levy, M.A.; Hirsch, J.D. Life Sci., 1983, 32, 2717-2723. “In Vitro and In Vivo Effects on Brain GABA Metabolism of (S)-4-Amino-5-fluoropentanoic Acid, A Mechanism-based Inactivator of γ-Aminobutyric Acid Transaminase.”
43. Silverman, R.B. J. Biol. Chem., 1983, 258, 14766-14769. “Mechanism of Inactivation of Monoamine Oxidase by trans-2-Phenylcyclopropylamine and the Structure of the Enzyme-Inactivator Adduct.”
44. Silverman, R.B.; Hoffman, S.J. Med. Res. Rev., 1984, 4, 415-447. “The Organic Chemistry of Mechanism-Based Enzyme Inhibition: A Chemical Approach to Drug Design.”
45. Silverman, R.B.; Yamasaki, R.B. Biochemistry, 1984, 23, 1322-1332. “Mechanism-based Inactivation of Mitochondrial Monoamine Oxidase by N-(1-Methylcyclopropyl)benzylamine.”
46. Silverman, R.B. Biochemistry, 1984, 23, 5206-5213. “Effect of a-Methylation on the Inactivation of Monoamine Oxidase by N-Cyclopropylbenzylamine.”
47. Silverman, R.B.; Tan, J.L. J. Org. Chem., 1984, 49, 4560-4562, “Mechanism for the Reaction of trans-2-Phenylcyclopropylamine with Nitrous Acid.”
48. Silverman, R.B.; Zieske, P.A. Biochemistry, 1985, 24, 2128-2138, “Mechanism of Inactivation of Monoamine Oxidase by 1-Phenylcyclopropylamine.”
49. Mukharji, I.; Silverman, R.B. Proc. Natl. Acad. Sci. (USA), 1985, 82, 2713-2717, “Purification of a Vitamin K Epoxide Reductase Which Catalyzes the Conversion of Vitamin K 2,3-epoxide to 3-Hydroxy-2-methyl-3-phytyl-2,3-dihydronaphthoquinone.”
50. Mathew, J.; Invergo, B.J.; Silverman, R.B. Syn. Commun., 1985, 15, 377-383. “An Efficient Synthesis of 3-Amino-4-fluorobutanoic Acid, an Inactivator of GABA Transaminase.”
51. Silverman, R.B.; Zieske, P.A. J. Med. Chem., 1985, 28, 1953-1957. “1-Benzylcyclopropylamine and (1-Phenylcyclopropyl)methylamine, an Inactivator and a Substrate of Monoamine Oxidase.”
52. Vazquez, M.L.; Silverman, R.B. Biochemistry, 1985, 24, 6538-6543, “Revised Mechanism for Inactivation of Mitochondrial Monoamine Oxidase by N-Cyclopropylbenzylamine.”
53. Yamasaki, R.B.; Silverman, R.B. Biochemistry, 1985, 24, 6543-6550, “Mechanism for Reactivation of N-Cyclopropylbenzylamine-Inactivated Monoamine Oxidase by Amines.”
54. Silverman, R.B.; Hiebert, C.K.; Vazquez, M.L. J. Biol. Chem., 1985, 260, 14648-14652, “Inactivation of Monoamine Oxidase by Allylamine Does Not Result in Flavin Attachment.”
55. Silverman, R.B.; Durkee, S.C.; Invergo, B.J. J. Med. Chem., 1986, 29, 764-770. “4-Amino-2-(substituted methyl)-2-butenoic Acids: Substrates and Potent Inhibitors of γ-Aminobutyric Acid Aminotransferase.”
56. Silverman, R.B. in Protein Tailoring for Food and Medical Uses (R.E. Feeney and J.R. Whitaker, Eds.), Marcel Dekker, N.Y., 1986, Chapter 8, pp 215-241, “Mechanism-Based Enzyme Inactivators for Medical Uses.”
57. Silverman, R.B.; Zieske, P.A. Biochemistry, 1986, 25, 341-346, “1-Phenylcyclobutylamine, the First in a New Class of Monoamine Oxidase Inactivators. Further Evidence for a Radical Intermediate.”
58. Silverman, R.B.; Zieske, P.A. Biochem. Biophys. Res. Commun., 1986, 135, 154-159, “Identification of the Amino Acid Bound to the Labile Adduct Formed During Inactivation of Monoamine Oxidase by 1-Phenylcyclopropylamine.”
59. Silverman, R.B.; Invergo, B.J.; Mathew, J. J. Med. Chem., 1986, 29, 1840-1846, “Inactivation of γ-Aminobutyric Acid Aminotransferase by (S,E)-4-Amino-5-fluoropent-2-enoic Acid and Effect on the Enzyme of (E)-3-(1-Aminocyclopropyl)-2-propenoic Acid.”
60. Silverman, R.B.; Invergo, B.J. Biochemistry, 1986, 25, 6817-6820, “Mechanism of Inactivation of γ-Aminobutyrate Aminotransferase by 4-Amino-5-fluoropentanoic Acid. First Example of an Enamine Mechanism for a γ-Amino Acid with a Partition Ratio of O.”
61. Silverman, R.B.; Invergo, B.J.; Levy, M.A.; Andrew, C.R. J. Biol. Chem., 1987, 262, 3192-3195, “Substrate Stereospecificity and Active Site Topography of γ-Aminobutyric Acid Aminotransferase for β-Aryl-γ-aminobutyric Acid Analogues.”
62. Silverman, R.B.; Banik, G.M. J. Am. Chem. Soc., 1987, 109, 2219-2220, “(Aminoalkyl)trimethylsilanes. A New Class of Monoamine Oxidase Inactivators.”
63. Silverman, R.B.; Vadnere, M.K. Bioorg. Chem., 1987, 15, 328-332, “Aminoalkyltrimethylgermanes: The First Organogermanium Mechanism-Based Enzyme Inactivators. A New Class of Monoamine Oxidase Inactivators.”
64. Silverman, R.B.; Mukharji, I.; Nandi, D.L. in Current Advances in Vitamin K Research (J. W. Suttie, Ed.), Elsevier/North-Holland, New York, 1988, 65-74, “Solubilization, Partial Purification, Mechanism, and Inactivation of Vitamin K Epoxide Reductase.”
65. Silverman, R.B.; George, C. Biochem. Biophys. Res. Commun. 1988, 150, 942-946, “Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase by (S,E)-4-Amino-5-fluoropent-2-enoic Acid.”
66. Silverman, R.B. J. Enz. Inhib. 1988, 2, 73-90, “The Potential Use of Mechanism-Based Enzyme Inactivators in Medicine.”
67. Silverman, R.B. in Topics in Medicinal Chemistry (4th SCI-RSC Medicinal Chemistry Symposium; P. R. Leeming, Ed., Royal Society of Chemistry, London, 1988, pp. 73-100, “Enzyme Inhibition: Approaches to Drug Design.”
68. Silverman, R.B.; George, C. Biochemistry, 1988, 27, 3285-3289, “Inactivation of γ-Aminobutyric Acid Aminotransferase by (Z)-4-Amino-2-fluoro-2-butenoic Acid.”
69. Hiebert, C.K.; Silverman, R.B. J. Med. Chem., 1988, 31, 1566-1570, “1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) Analogues. Inactivation of Monoamine Oxidase by Conformationally-Rigid Analogues of N,N-Dimethylcinnamylamine.”
70. Silverman, R.B.; Hiebert, C.K. Biochemistry, 1988, 27, 8448-8453, “Inactivation of Monoamine Oxidase A by the Monoamine Oxidase B Inactivators 1-Phenylcyclopropylamine, 1-Benzylcyclopropylamine, and N-Cyclopropyl-β-methylbenzylamine.”
71. Silverman, R.B.; Nandi, D.L. Biochem. Biophys. Res. Commun. 1988, 155, 1248-1254, “Reduced Thioredoxin: A Possible Physiological Cofactor for Vitamin K Epoxide Reductase. Further Support for an Active Site Disulfide.”
72. Yelekci, K.; Lu, X.; Silverman, R.B. J. Am. Chem. Soc. 1989, 111, 1138-1140, “Electron Spin Resonance Studies of Monoamine Oxidase B. First Direct Evidence for a Substrate Radical Intermediate.”
73. Silverman, R.B.; Oliver, J. S. J. Med. Chem., 1989, 32, 2138-2141, “2-Fluoromethyl-3-phytyl-1,4-naphthoquinone and its 2,3-Epoxide. Inhibition of Vitamin K Epoxide Reductase.”
74. Andruszkiewicz, R.; Silverman, R.B. Synthesis, 1989, 953-955, “A Convenient Synthesis of 3-Alkyl-4-aminobutanoic Acids.”
75. Gates, K.S.; Silverman, R.B. J. Am. Chem. Soc., 1989, 111, 8891-8895, “Model Studies for the Mechanism of Inactivation of Monoamine Oxidase by 5-Aminomethyl-3-aryl-2-oxazolidinones.”
76. Nanavati, S.M.; Silverman, R.B. J. Med. Chem., 1989, 32, 2413-2421, “Design of Potential Anticonvulsant Agents: Mechanistic Classification of γ-Aminobutyric Acid Aminotransferase Inactivators.”
77. Hiebert, C.K.; Sayre, L.M.; Silverman, R.B. J. Biol. Chem., 1989, 264, 21516-21521, “Inactivation of Monoamine Oxidase by 3,3-Dimethyl Analogues of 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and 1-Methyl-4-phenyl-2,3-dihydropyridinium Ion (MPDP+). Dramatic effect of β-Mercaptoethanol on Substrate Turnover and Enzyme Inactivation.”
78. Silverman, R.B.; Nanavati, S.M. J. Med. Chem., 1990, 33, 931-936, “Selective Inhibition of γ-Aminobutyric Acid Aminotransferase by (3R,4R),(3S,4S) and (3R,4S),(3S,4R)-4-Amino-5-fluoro-3-phenylpentanoic Acids.”
79. Andruszkiewicz, R.; Barrett, A.G.M.; Silverman, R.B. Syn. Commun., 1990, 20, 159-166, “Chemoenzymatic Synthesis of (R)- and (S)-4-Amino-3-methylbutanoic Acids.”
80. Ryall, R.P.; Silverman, R.B. Syn. Commun., 1990, 20, 431-438, “Synthesis of 2-Substituted-3-phytyl-1,4-naphthoquinone Epoxides.”
81. Banik, G.M.; Silverman, R.B. J. Am. Chem. Soc., 1990, 112, 4499-4507, “Mechanism of Inactivation of Monoamine Oxidase B by (Aminomethyl)trimethylsilane.”
82. Silverman, R.B.; Nandi, D.L. J. Enz. Inhib. 1990, 3, 289-294, “Effect of N-Ethylmaleimide on Beef and Rat Liver Vitamin K1 Epoxide Reductase.”
83. Ryall, R.P.; Nandi, D.L.; Silverman, R.B. J. Med. Chem., 1990, 33, 1790-1797, “Substituted Vitamin K Epoxide Analogues. New Competitive Inhibitors and Substrates of Vitamin K1 Epoxide Reductase.”
84. Gates, K.S.; Silverman, R.B. J. Am. Chem. Soc., 1990, 112, 9364-9372, “5-(Aminomethyl)-3-aryl-2-oxazolidinones. A Novel Class of Mechanism-Based Inactivators of Monoamine Oxidase B.”
85. Andruszkiewicz, R.; Silverman, R.B. J. Biol. Chem., 1990, 265, 22288-22291, “4-Amino-3-alkylbutanoic Acids as Substrates for γ-Aminobutyric Acid Aminotransferase.”
86. Silverman, R.B. Biochem. Soc. Trans., 1991, 19, 201-206, “The Use of Mechanism-Based Inactivators to Probe the Mechanism of Monoamine Oxidase.”
87. Silverman, R.B.; Andruszkiewicz, R.; Nanavati, S.M.; Taylor, C.P.; Vartanian, M.G. J. Med. Chem., 1991, 34, 2295-2298. “3-Alkyl-4-aminobutyric Acids: The First Class of Anticonvulsant Agents That Activates L-Glutamic Acid Decarboxylase.”
88. Burke, J.R.; Silverman, R.B. J. Enz. Inhib., 1991, 5, 199-205. “4-(Oxoalkyl)-substituted GABA Analogues as Inactivators and Substrates of GABA Aminotransferase.”
89. Burke, J.R.; Silverman, R.B. J. Am. Chem. Soc., 1991, 113, 9329-9340. “Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase by 4-Amino-5-hexynoic Acid (γ-Ethynyl GABA).”
90. Nanavati, S.M.; Silverman, R.B. J. Am. Chem. Soc., 1991, 113, 9341-9349. “Mechanisms of Inactivation of γ-Aminobutyric Acid Aminotransferase by the Antiepilepsy Drug γ-Vinyl GABA (Vigabatrin).”
91. Taylor, C.P.; Vartanian, M.G.; Andruszkiewicz, R.; Silverman, R.B. Epilepsy Res. 1992, 11, 103-110. “3-Alkyl GABA and 3-Alkylglutamate Analogues: Two New Classes of Anticonvulsant Agents.”
92. Ding, Z.; Silverman, R.B. J. Med. Chem. 1992, 35, 885-889. “5-(Aminomethyl)-3-aryldihydrofuran-2(3H)-ones, a New Class of Monoamine Oxidase-B Inactivators.”
93. Silverman, R.B. In Advances in Electron Transfer Chemistry, Vol. 2; Mariano, P.S., Ed.; JAI Press: Greenwich, CT, 1992; pp. 177-213. “Electron Transfer Chemistry of Monoamine Oxidase.”
94. Hopkins, M.H.; Silverman, R.B. J. Enz. Inhib. 1992, 6, 125-129. “β-Lactams: A New Class of Conformationally-Rigid Inhibitors of γ-Aminobutyric Acid Aminotransferase.”
95. Hopkins, M.H.; Silverman, R.B. BioMed. Chem. Lett. 1992, 2, 1371-1374. “α-Amino Acid Analogues as Mechanism-Based Inactivators of γ-Aminobutyric Acid Aminotransferase.”
96. Hopkins, M.H.; Bichler, K.A.; Su, T.; Chamberlain, C.L.; Silverman, R.B. J. Enz. Inhib. 1992, 6, 195-199. “Inactivation of γ-Aminobutyric Acid Aminotransferase by Various Amine Buffers.”
97. Ding, C.Z.; Silverman, R.B. J. Enz. Inhib. 1992, 6, 223-231. “4-(Aminomethyl)-1-Aryl-2-pyrrolidinones, a New Class of Monoamine Oxidase B Inactivators.”
98. Zelechonok, Y.; Silverman, R.B. J. Org. Chem. 1992, 57, 5785-5787. “Mechanism for the Reaction of Tributyltin Radicals with Aldehydes.”
99. Zelechonok, Y.; Silverman, R.B. J. Org. Chem. 1992, 57, 5787-5790. “Silver (I)/Peroxydisulfate-Induced Oxidative Decarboxylation of Amino Acids. A Chemical Model for a Possible Intermediate in the Monoamine Oxidase-Catalyzed Oxidation of Amines.”
100. Silverman, R.B.; Zelechonok, Y. J. Org. Chem. 1992, 57, 6373-6374. “Evidence for a Hydrogen Atom Transfer Mechanism or a Proton/Fast Electron Transfer Mechanism for Monoamine Oxidase.”
101. Silverman, R.B.; Lu, X.L.; Banik, G.M. J. Org. Chem. 1992, 57, 6617-6622. “Formylsilanes. Chemoenzymatic and Chemical Syntheses of the 2,4-Dinitrophenylhydrazones of These Apparently Air- and Water-Stable Compounds.”
102. Silverman, R.B.; Ding, C.Z.; Gates, K.S. Perspectives in Medicinal Chemistry ; Testa, B.; Kyburz, E.; Fuhrer, W.; Giger, R., Eds.; Verlag Helvetica Chimica Acta: Basel; 1993, 73-86. “Design and Mechanism of Monoamine Oxidase Inactivators from a Chemical Perspective.”
103. Silverman, R.B.; Nishimura, K.; Lu, X. J. Am. Chem. Soc. 1993, 115, 4949-4954. “Mechanism of Inactivation of Monoamine Oxidase-B by the Anticonvulsant Agent Milacemide (2-(n-Pentylamino)acetamide).”
104. Silverman, R.B.; Ding, C.Z.; Borrillo, J.L.; Chang, J.T. J. Am. Chem. Soc. 1993, 115, 2982-2983. ” Mechanism-Based Enzyme Inactivation via a Diactivated Cyclopropane Intermediate.”
105. Nishimura, K.; Lu, X.; Silverman, R.B. J. Med. Chem. 1993, 36, 446-448. “Inactivation of Monoamine Oxidase B by Analogues of the Anticonvulsant Agent Milacemide (2-n-Pentylaminoacetamide).”
106. Silverman, R.B.; Cesarone, J.M.; Lu, X. J. Am. Chem. Soc. 1993, 115, 4955-4961. “Stereoselective Ring Opening of 1-Phenylcyclopropylamine Catalyzed by Monoamine Oxidase-B.”
107. Silverman, R. B.; Ding, C.Z. J. Am. Chem. Soc. 1993, 115, 4571-4576. “A Chemical Model for the Mechanism of Inactivation of Monoamine Oxidase by Heterocyclic Compounds. Electronic Effects on Acetal Hydrolysis”
108. Lu, X.; Silverman, R.B. J. Enz. Inhib. 1993, 7, 43-45. “The Antiulcer Drug Ranitidine Hydrochloride and its Synthetic Intermediates are Inactivators of Monoamine Oxidase-B.”
109. Ding, C.Z.; Silverman, R.B. Syn. Commun. 1993, 23, 1467-1471. “Synthesis of N-Carbobenzoxy-N,N-acetals.”
110. Ding, C.Z.; Lu, X.; Nishimura, K.; Silverman, R.B. J. Med. Chem., 1993, 36, 1711-1715. “Transformation of Monoamine Oxidase-B Primary Amine Substrates into Time-Dependent Inhibitors. Tertiary Amine Homologues of Primary Amine Substrates.”
111. Silverman, R.B.; Tran, N.; Sinha, R.K.; Neuhaus, F.C. Biochem. Biophys. Res. Commun. 1993, 195, 1077-1080. “The Oxazolidinone Antibacterial Agent DuP 105 Does Not Act on Cell Wall Biosynthesis or on a β-Lactamase.”
112. Ding, C. Z.; Silverman, R. B. BioMed. Chem. Lett. 1993, 3, 2077-2078. “Selective Inactivation of Monoamine Oxidase B by Aminoethyl 3-Chlorobenzyl Ether.”
113. Silverman, R. B.; Zhou, J. P.; Eaton, P. E. J. Am. Chem. Soc. 1993, 115, 8841-8842. “Inactivation of Monoamine Oxidase by (Aminomethyl)cubane. First Evidence for an α-Amino Radical During Enzyme Catalysis.”
114. Ding, C. Z.; Silverman, R. B. J. Med. Chem. 1993, 36, 3606-3610. “Transformation of Heterocyclic Reversible Monoamine Oxidase-B Inactivators into Irreversible Inactivators by N-Methylation.”
115. Annan, N.; Silverman, R. B. J. Med. Chem., 1993, 36, 3968-3970. “New Analogues of N-(2-Aminoethyl)-4-chlorobenzamide (Ro 16-6491). Some of the Most Potent Monoamine Oxidase-B Inactivators.”
116. Silverman, R. B.; Lu, X. J. Am. Chem. Soc. 1994, 116, 4129-4130. “Evidence Against a Nucleophilic Mechanism for Monoamine Oxidase-Catalyzed Amine Oxidation.”
117. Woo, J. C. G.; Silverman, R. B. Biochem. Biophys. Res. Commun. 1994, 202, 1574-1578. “Observation of Two Different Chromophores in the Resting State of Monoamine Oxidase B by Fluorescence Spectroscopy.”
118. Silverman, R. B.; Lu, X.; Zhou, J. J. P.; Swihart, A. J. Am. Chem. Soc. 1994, 116, 11590-11591. “Monoamine Oxidase B-Catalyzed Oxidation of Cinnamylamine-2,3-oxide. Further Evidence against a Nucleophilic Mechanism.”
119. Silverman, R. B.; Olson, G. T. Bioorg. Med. Chem., 1995, 3, 11-18. “Inactivation of γ-Aminobutyric Acid Aminotransferase by L-3-Chloroalanine Hydroxamate.”
120. Silverman, R. B. Methods Enzymol. 1995, 249, 240-283. “Mechanism-Based Enzyme Inactivators.”
121. Silverman, R. B.; Hawe, W. P. J. Enz. Inhib., 1995, 9, 203-215. “SAR Studies of Fluorine-Substituted Benzylamines and Substituted 2-Phenylethylamines as Substrates and Inactivators of Monoamine Oxidase B.”
122. Silverman, R. B. Prog. Brain Res. 1995, 106, 23-31. “Radical Thoughts about the Life of MAO.”
123. Woo, J. C. G.; Silverman, R. B. J. Am. Chem. Soc., 1995, 117, 1663-1664. “Monoamine Oxidase B Catalysis in Low Aqueous Medium. Direct Evidence for an Imine Product.”
124. Zhou, J. J. P.; Zhong, B.; Silverman, R. B. J. Org. Chem. 1995, 60, 2261-2262. “Improved Procedure for the Synthesis of Substituted β-Hydroxynitriles.”
125. Lightcap, E. S.; Hopkins, M. H.; Olson, G. T.; Silverman, R. B. Bioorg. Med. Chem. 1995, 3, 579-585. “Time-Dependent Inhibition of γ-Aminobutyric Acid Aminotransferase by 3-Hydroxybenzylhydrazine.”
126. Silverman, R. B.; Olson, G. T. J. Org. Chem. 1995, 60, 6232-6234. “Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase by 3-Hydrazinopropionic Acid.”
127. Woo, J. C. G.; Wang, X.; Silverman, R. B. J. Org. Chem. 1995, 60, 6235-6236. “Monoamine Oxidase-Catalyzed Amine Oxidation in Organic Solvents.”
128. Silverman, R. B. Acc. Chem. Res. 1995, 28, 335-342. “Radical Ideas About Monoamine Oxidase.”
129. Silverman, R. B.; Zhou, J. J. P.; Ding, C. Z.; Lu, X. J. Am. Chem. Soc. 1995, 117, 12895- 12896. “Monoamine Oxidase-Catalyzed Oxidative Decarboxylation of cis– and trans-5- Aminomethyl-3-(4-methoxyphenyl)dihydrofuran-2(3H)-one. Evidence for the Intermediacy of an α-Radical.”
130. Lightcap, E. S.; Silverman, R. B. J. Med. Chem. 1996, 39, 686-694. “Slow-binding Inhibition of γ-Aminobutyric Acid Aminotransferase by Hydrazine Analogues.”
131. Zhou, J. J. P.; Zhong, B.; Silverman, R. B. Anal. Biochem. 1996, 234, 9-12. “Direct Continuous Fluorometric Assay for Monoamine Oxidase B.”
132. Silverman, R. B.; Bichler, K. A.; Leon, A. J. J. Am. Chem. Soc. 1996, 118, 1241-1252. “Mechanisms of Inactivation of γ-Aminobutyric Acid Aminotransferase by 4-Amino-5-fluoro-5-hexenoic Acid.”
133. Silverman, R. B.; Bichler, K. A.; Leon, A. J. J. Am. Chem. Soc. 1996, 118, 1253-1261. “Unusual Mechanistic Difference in the Inactivation of γ-Aminobutyric Acid Aminotransferase by (E)- and (Z)-4-Amino-6-fluoro-5-hexenoic Acids.”
134. Silverman, R. B.; Olson, G. T. Bioorg. Med. Chem. Lett. 1996, 6, 143-146. “3-Substituted Alanines Inactivate γ-Aminobutyric Acid Aminotransferase by the Same Mechanism as do 4-Amino-5-halopentanoic Acid Analogues.”
135. Silverman, R. B.; Roscher, C. L.C. Bioorg. Med. Chem. 1996, 4, 1521-1535. “Mechanism-Based Inactivation of γ-Aminobutyric Acid Aminotransferase by 3-Amino-4-fluorobutanoic Acid.”
136. Leon, A. J.; Silverman, R. B. Bioorg. Med. Chem. Lett. 1996, 6, 1319-1322. “Inactivation of γ-Aminobutyric Acid Aminotransferase by (Z)-4-Amino-6-fluoro-5-hexenoic Acid: Identification of an Active Site Residue.”
137. DeRose, V.J.; Woo, J.C.G.; Hawe, W.P.; Hoffman, B.M.; Silverman, R.B.; Yelekci, K. Biochemistry 1996, 35, 11085-11091. “Characterization of a Flavin Semiquinone in the Resting State of Monoamine Oxidase B by Electron Paramagnetic Resonance and Electron Nuclear Double Resonance Spectroscopy.”
138. Silverman, R. B. In Contemporary Enzyme Kinetics and Mechanism, 2nd edition; Purich, D. L., ed.; Academic Press: San Diego, 1996, pp. 291-334. “Mechanism-Based Enzyme Inactivators.”
139. Lu, X.; Yang, S.; Silverman, R.B. J. Org. Chem., 1996, 61, 8961-8966. “Monoamine Oxidase-Catalyzed Oxidative Rearrangement of trans, trans-1-(Aminomethyl)-2-methoxy-3-phenylcyclopropane.”
140a. Silverman, R. B.; Lu, X.; Blomquist, G.; Ding, C. Z.; Yang, S. Bioorg. Med. Chem. 1997,5, 297-304. “Inactivation of Monoamine Oxidase B by Benzyl 1-(Aminomethyl)cyclopropane-1-carboxylate.”
140b. Silverman, R. B.; Lu, X.; Blomquist, G.; Ding, C. Z.; Yang, S. Bioorg. Med. Chem. 1998,6, 365. Corrigendum to “Inactivation of Monoamine Oxidase B by Benzyl 1-(Aminomethyl)cyclopropane-1-carboxylate.”
141. Zhou, J. P.; Li, J.; Upadhyaya, S.; Eaton, P. E.; Silverman, R. B. J. Med. Chem. 1997, 40, 1165-1168. “4-Substituted Cubylcarbinyl Amines: A New Class of Mechanism-Based Monoamine Oxidase B Inactivators.”
142. Silverman, R. B. Il Farmaco, 1997, 52, 343-352. “Oxazolidinones, Dihydrofuranones, and Pyrrolidinones as Inactivators and Substrates of Monoamine Oxidase B: Approaches to the Design of Antiparkinsonian Agents.”
143. Fast, W.; Levsky, M. E.; Marletta, M. A.; Silverman, R. B., Bioorg. Med. Chem. 1997, 5, 1601-1608. “Nω-Propargyl-L-arginine and Nω-Hydroxy-Nω-propargyl-L-arginine are Inhibitors, but Not Inactivators, of Neuronal and Macrophage Nitric Oxide Synthases.”
144. Fast, W.; Huff, M. E.; Silverman, R. B. Bioorg. Med. Chem. Lett. 1997, 7, 1449-1454. “Time-Dependent Inhibition of Neuronal Nitric Oxide Synthase by N-Propargylguanidine.”
145. Zhong, B.; Silverman, R. B. J. Am. Chem. Soc. 1997, 119, 6690-6691. “Identification of the Active Site Cysteine in Bovine Liver Monoamine Oxidase B.”
146. Silverman, R. B.; Huang, H.; Marletta, M. A.; Martasek, P. J. Med. Chem. 1997, 40, 2813-2817. “Selective Inhibition of Neuronal Nitric Oxide Synthase by Nω-Nitroarginine- and Phenylalanine-Containing Dipeptides and Dipeptide Esters.”
147. Zhang, H. Q.; Dixon, R. P.; Marletta, M. A.; Nikolic, D.; Van Breemen, R.; Silverman, R. B., J. Am Chem. Soc. 1997, 119, 10888-10902. “Mechanism of Inactivation of Neuronal Nitric Oxide Synthase by Nω-Allyl-L-arginine.”
148. Zhang, H. Q.; Fast, W.; Marletta, M. A.; Martasek, P.; Silverman, R. B. J. Med. Chem. 1997, 40, 3869-3870. “Potent and Selective Inhibition of Neuronal Nitric Oxide Synthase by Nω-Propyl-L-arginine.”
149. Olson, G. T.; Fu, M.; Lau, S.; Rinehart, K. L.; Silverman, R. B., J. Am. Chem. Soc. 1998, 120, 2256-2267. “An Aromatization Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase for the Antibiotic L-Cycloserine.”
150. Yelekçi, K.; Silverman, R. B., J. Enzyme Inhib. 1998, 13, 31-39. “Effect of the Locus of the Oxygen Atom in Amino Ethers on the Inactivation of Monoamine Oxidase B.”
151. Lu, X.; Silverman, R. B. Bioorg. Med. Chem. 1998, 6, 1851-1856. “Inactivation of Monoamine Oxidase B by cis– and trans-5-Aminomethyl-3-(4-methoxyphenyl)dihydrofuran-2(3H)-ones.”
152. Lu, X.; Silverman, R. B. J. Am. Chem. Soc. 1998, 120, 10583-10587. “Monoamine Oxidase B-Catalyzed Reactions of cis– and trans-5-Aminomethyl-3-(4-methoxyphenyl)dihydrofuran-2(3H)-ones. Evidence for a Reversible Redox Reaction.”
153. Wang, X.; Silverman, R. B. J. Org. Chem. 1998, 63, 7357-7363. “2-(Iodoethenyl)benzyl Amines as Potential Probes for Radical Intermediates Formed During Monoamine Oxidase-Catalyzed Oxidations.”
154. Zhong, B.; Lu, X.; Silverman, R. B. Bioorg. Med. Chem. 1998, 6, 2405-2419. “Syntheses of Amino Nitrones. Potential Intramolecular Traps for Radical Intermediates in Monoamine Oxidase-Catalyzed Reactions.”
155. Fast, W.; Nikolic, D.; Van Breemen, R.; Silverman, R. B. J. Am. Chem. Soc. 1999, 121, 903-916. “Mechanism of Inactivation of Inducible Nitric Oxide Synthase by N5-(1-Iminoethyl)-L-ornithine (L-NIO).”
156. Lee, Y.; Marletta, M. A.; Martasek, P.; Roman, L. J.; Masters, B. S. S.; Silverman, R. B. Bioorg. Med. Chem., 1999, 7, 1097-1104. “Conformationally-restricted Arginine Analogues as Alternative Substrates and Inhibitors of Nitric Oxide Synthases.”
157. Qiu, J.; Stevenson, S. H.; O’Beirne, M. J.; Silverman, R. B. J. Med. Chem. 1999, 42, 329-332. “2,6-Difluorophenol as a Bioisostere of a Carboxylic Acid: Bioisosteric Analogues of γ-Aminobutyric Acid.”
158. Tierney, D. L.; Huang, H.; Martasek, P.; Masters, B. S. S.; Silverman, R. B.; Hoffman, B. M. Biochemistry 1999, 38, 3704-3710. “ENDOR Spectroscopic Evidence for the Position and Structure of NG-Hydroxy-L-arginine Bound to holo-Neuronal Nitric Oxide Synthase.”
159. Johnson, T. R.; Silverman, R. B. Bioorg. Med. Chem. 1999, 7, 1625-1636. “Syntheses of (Z)- and (E)-4-Amino-2-(trifluoromethyl)-2-butenoic Acid and Their Inactivation of γ-Aminobutyric Acid Aminotransferase.”
160. Fu, M.; Silverman, R. B. Bioorg. Med. Chem. 1999, 7, 1581-1590. “Isolation and Characterization of the Product of Inactivation of γ-Aminobutyric Acid Aminotransferase by Gabaculine.”
161. Huang, H.; Martasek, P.; Roman, L. J.; Masters, B. S. S.; Silverman, R. B. J. Med. Chem. 1999, 42, 3147-3153. “Nω-Nitroarginine-Containing Dipeptide Amides. Potent and Highly Selective Inhibitors of Neuronal Nitric Oxide Synthase.”
162. Lee, Y.; Martasek, P.; Roman, L. J.; Masters, B. S. S.; Silverman, R. B. Bioorg. Med. Chem. 1999, 7, 1941-1951. “Imidazole-Containing Amino Acids as Selective Inhibitors of Nitric Oxide Synthases.”
163. Lee, Y.; Silverman, R. B. Synthesis 1999, 1495-1499. “Solid-Phase Syntheses of Nω-Propylarginine-Containing Dipeptides, Dipeptide Esters, and Dipeptide Amides.”
164. Fu, M.; Nikolic, D.; Van Breemen, R.; Silverman, R. B. J. Am. Chem. Soc. 1999, 121, 7751-7759. “Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase by (S)-4-Amino-4,5-dihydro-2-thiophenecarboxylic Acid.”
165. Lee, Y.; Silverman, R. B. J. Am. Chem. Soc. 1999, 121, 8407-8408. “Efficient Solid-Phase Synthesis of Compounds Containing Phenylalanine and its Derivatives via Side-Chain Attachment to the Polymer Support.”
166. Qiu, J.; Pingsterhaus, J. M.; Silverman, R. B. J. Med. Chem. 1999, 42, 4725-4728. “Inhibition and Substrate Activity of Conformationally-Rigid Vigabatrin Analogues with γ-Aminobutyric Acid Aminotransferase.”
167. Woodroofe, C. C.; Mostashari, R.; Lu, X.; Ramsay, R. R.; Silverman, R. B. J. Enzyme Inhib. 1999, 15, 11-21. “Selective Inhibition of Monoamine Oxidase B by Aminoethyl Substituted Benzyl Ethers.”
168. Chebib, M.; Johnston, G. A. R.; Mattsson, J. P.; Rydström, K., Nilsson, K.; Qiu, J.; Stevenson, S. H.; Silverman, R. B. Bioorg. Med. Chem. Lett. 1999, 9, 3093-3098. “Aminomethyl-2,6-difluorophenols as a Novel Class of Increased Lipophilicity GABAC Receptor Antagonists.”
169. Tantillo, D.; Fukuto, J. M.; Hoffman, B. M.; Silverman, R. B.; Houk, K. N. J. Am. Chem. Soc. 2000, 122, 536-537. “Theoretical Studies on NG-Hydroxy-L-arginine and Derived Radicals: Implications for the Mechanism of Nitric Oxide Synthase.”
170. Koo, Y. K.; Nandi, D.; Silverman, R. B. Arch. Biochem. Biophys. 2000, 374, 248-254. “Multiple Active Enzyme Species of γ-Aminobutyric Acid Aminotransferase are not Isozymes, but are Proteolytic Fragments.”
171. Woodroofe, C. C.; Zhong, B.; Lu, X.; Silverman, R. B. J. Chem. Soc. Perkin Trans. 2 2000, 55-60. “Anomalous Schmidt Reaction Products of Phenylacetic Acid and Derivatives.”
172. Qiu, J.; Silverman, R. B. J. Med. Chem. 2000, 43, 706-720. “A New Class of Conformationally-Rigid Analogues of 4-Amino-5-halopentanoic Acids, Potent Inactivators of γ-Aminobutyric Acid Aminotransferase.”
173. Lee, Y.; Silverman, R. B. Organic Lett. 2000, 2, 303-306. “Traceless Solid-Phase Synthesis of Chiral 3-Aryl β-Amino Acid-Containing Peptides Using a Side Chain Tethered β-Amino Acid Building Block.”
174. Wang, X.; Silverman, R. B. Bioorg. Med. Chem. 2000, 8, 1645-1651. “Monoamine Oxidase-Catalyzed Oxidation of endo, endo-2-Amino-6-[(Z)-2′-phenyl]ethenylbicyclo[2.2.1]heptane, a Potential Probe for a Radical Cation Intermediate.”
175. Tierney, D. L.; Huang, H.; Martásek, P.; Roman, L. J.; Silverman, R. B.; Masters, B. S. S.; Hoffman, B. M. J. Am. Chem. Soc. 2000, 122, 5405-5406. “ENDOR Studies of L-Arginine and NG-Hydroxy-L-Arginine Bound to All Three Holo-Nitric Oxide Synthase Isozymes.”
176. Huang, H.; Martásek, P.; Roman, L. J.; Silverman, R. B. J. Med. Chem. 2000, 43, 2938-2945. “Synthesis and Evaluation of Peptidomimetics as Selective Inhibitors and Active Site Probes of Nitric Oxide Synthases.”
177. Tierney, D. L.; Huang, H.; Martásek, P.; Roman, L. J.; Silverman, R. B.; Hoffman, B. M. J. Am. Chem. Soc. 2000, 122, 7869-7875. “ENDOR Spectroscopic Evidence for the Geometry of Binding of retro-inverso-Nω-Nitroarginine-Containing Dipeptide Amides to Neuronal Nitric Oxide Synthase.”
178. Hah, J. M.; Roman, L. J.; Silverman, R. B. Bioorg. Med. Chem. 2000, 8, 1931-1936. “Deuterium Isotope Effects and Product Studies for the Oxidation of Nω-Allyl-L-arginine and Nω-Allyl-Nω-hydroxy-L-arginine by Neuronal Nitric Oxide Synthase.”
179. Lee, Y.; Silverman, R. B. Organic Lett. 2000, 2, 3743-3746. “Rapid, High-Yield, Solid-Phase Synthesis of the Antitumor Antibiotic Sansalvamide A Using a Side-Chain-Tethered Phenylalanine Building Block.”
180. Lee, Y.; Martásek, P.; Roman, L. J.; Silverman, R. B. Bioorg. Med. Chem. Lett. 2000, 10, 2771-2774 “1-H-Pyrazole-1-carboxamidines: New Inhibitors of Nitric Oxide Synthase.”
181. Mitchell, D. J.; Nikolic, D.; Rivera, E.; Sablin, S. O.; Choi, S.; van Breemen, R. B.; Singer, T. P.; Silverman, R. B. Biochemistry 2001, 40, 5447-5456. “Spectrometric Evidence for the Flavin-1-phenylcyclopropylamine Inactivator Adduct with Monoamine Oxidase N.”
182. Huang, H.; Martásek, P.; Roman, L. J.; Silverman, R. B. J. Enzyme Inhib. 2001, 16, 233-239. “Synthesis and Evaluation of Dipeptide Amides Containing Nω-Nitroarginine and D-2,4-Diaminobutyric Acid as Inhibitors of Neuronal Nitric Oxide Synthase.”
183. Huang, H.; Hah, J.-M.; Silverman, R. B. J. Am. Chem. Soc. 2001, 123, 2674-2676. “Mechanism of Nitric Oxide Synthase. Evidence that Direct Hydrogen Atom Abstraction from the O-H Bond of NG-Hydroxyarginine is Not Relevant to the Mechanism.”
184. Mitchell, D. J.; Nikolic, D.; van Breemen, R. B.; Silverman, R. B. Bioorg. Med. Chem. Lett., 2001, 11, 1757-1760. “Inactivation of Monoamine Oxidase B by 1-Phenylcyclopropylamine: Mass Spectral Evidence for the Flavin Adduct.”
185. Mitchell, D. J.; Nikolic, D.; Jang, M.-H.; van Breemen, R. B.; Hille, R.; Silverman, R. B. Biochemistry 2001, 40, 8523-8530. “Inactivation of C30A Trimethylamine Dehydrogenase by N-Cyclopropyl-α-methylbenzylamine, 1-Phenylcyclopropylamine, and Phenylhydrazine.”
186. Lee, Y.; Silverman, R. B. Tetrahedron 2001, 57, 5339-5352. “Silicon-Based Aromatic Transferring Linkers for Traceless Solid-Phase Synthesis of Aryl-, Polyaryl-, and Heteroaryl-Containing Compounds.”
187. Hah, J.-M.; Roman, L. J.; Martásek, P.; Silverman, R. B. J. Med. Chem. 2001, 44, 2667-2670. “Reduced Amide Bond Peptidomimetics. (4S)-N-(4-Amino-5-[aminoalkyl]aminopentyl)-N‘-nitroguanidines, Potent and Highly Selective Inhibitors of Neuronal Nitric Oxide Synthase.”
188. Gómez-Vidal, J. A.; Forrester, M. T.; Silverman, R. B. Organic Lett. 2001, 3, 2477-2479. “Mild and Selective Sodium Azide-Mediated Cleavage of p-Nitrobenzoic Esters.”
189. Gómez-Vidal, J. A.; Silverman, R. B. Organic Lett. 2001, 3, 2481-2484. “Short, Highly Efficient Syntheses of 3-Azido- and 4-Azidoproline Derivatives and Their Precursors.”
190. Choi, S.; Storici, P.; Schirmer, T.; Silverman, R. B. J. Am. Chem. Soc. 2002, 124, 1620-1624. “Design of a Conformationally-Restricted Analogue of the Antiepilepsy Drug Vigabatrin that Directs its Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase.”
191. Choi, S.; Silverman, R. B. J. Med. Chem. 2002, 45, 4531-4539. “Inactivation and Inhibition of γ-Aminobutyric Acid Aminotransferase by Conformationally-Restricted Vigabatrin Analogues.”
192. Lu, X.; Rodriguez, M.; Ji, H.; Silverman, R. B.; Vintém, A. P. B.; Ramsay, R. R. “Irreversible Inactivation of Mitochondrial Monoamine Oxidases” In Flavins and Flavoproteins 2002: Proceedings of the 14th International Symposium; Chapman, S. K.; Perham, R. N.; Scrutton, N. S., Eds.; Rudolf Weber: Berlin, Germany, 2002; pp 817-830.
193. Gu, W.; Liu, S.; Silverman, R. B. Organic Lett. 2002, 4, 4171-4174. “Solid-Phase, Pd-Catalyzed, Silicon-Aryl Carbon Bond Formation. Synthesis of Sansalvamide A Peptide.”
194. Lee, Y.; Ling, K.-Q.; Lu, X.; Silverman, R. B.; Shepard, E. M.; Dooley, D. M.; Sayre, L. M. J. Am. Chem. Soc. 2002, 124, 12135-12143. “3-Pyrrolines are Mechanism-Based Inactivators of the Quinone-Dependent Amine Oxidases but Only Substrates of the Flavin-Dependent Amine Oxidases.”
195. Nandi, D.; Lightcap, E. S.; Koo, Y. K.; Lu, X.; Quancard, J.; Silverman, R. B. Int. J. Biochem. Cell Biol., 2003, 35, 1085-1097. “Purification and Inactivation of 3-Hydroxyanthranilic Acid 3,4-Dioxygenase from Beef Liver.”
196. Gu, W.; Silverman, R. B. Organic Lett. 2003, 5, 415-418. “New Stable Backbone Linker Resins for Solid-Phase Peptide Synthesis.”
197. Hah, J.-M.; Martásek, P.; Roman, L. J.; Silverman, R. B. J. Med. Chem. 2003, 46, 1661-1669.”Aromatic Reduced Amide Bond Peptidomimetics as Selective Inhibitors of Neuronal Nitric Oxide Synthase.”
198. Lu, X.; Rodríguez, M.; Gu, W.; Silverman, R. B. Bioorg. Med. Chem. 2003, 11, 4423-4430. “Inactivation of Mitochondrial Monoamine Oxidase B by Methylthio-Substituted Benzylamines.”
199. Lu, X.; Nikolic, D.; Mitchell, D. J.; van Breemen, R. B.; Mersfelder, J. A.; Hille, R.; Silverman, R. B. Bioorg. Med. Chem. Lett. 2003, 13, 4129-4132 . “A Mechanism for Substrate-Induced Formation of 6-Hydroxyflavin Mononucleotide Catalyzed by C30A Trimethylamine Dehydrogenase.”
200. Gu, W.; Silverman, R. B. J. Org. Chem. 2003, 68, 8774-8779. “Solid-Phase Total Synthesis of Scytalidamide A.”
201. Ji, H.; Li, H.; Flinspach, M.; Poulos, T. L.; Silverman, R. B. J. Med. Chem., 2003, 46, 5700-5711. “Computer Modeling of Selective Regions in the Active Site of Nitric Oxide Synthases: Implication for the Design of Isoform-Selective Inhibitors.”
202. Pan, Y.; Qiu, J.; Silverman, R. B. J. Med. Chem. 2003, 46, 5292-5293. “Design, Synthesis, and Biological Activity of a Difluoro-substituted, Conformationally-rigid Vigabatrin Analogue As a Potent γ-Aminobutyric Acid Aminotransferase Inhibitor.”
203. Flinspach, M.; Li, H.; Jamal, J.; Yang, W.; Huang, H.; Hah, J.-M.; Gomez-Vidal, J. A.; Litzinger, E. A.; Silverman, R. B.; Poulos, T. L. Nature (Struct. Mol. Biol.) 2004, 11, 54-59. “Structural Basis for Dipeptide Amide Isoform-Selective Inhibition of Neuronal Nitric Oxide Synthase.”
204. Fu, M.; Silverman, R. B. Bioorg. Med. Chem. Lett. 2004, 14, 203-206. “Inactivation of γ-Aminobutyric Acid Aminotransferase by (S)-4-Amino-4,5-dihydro-2-furancarboxylic Acid Does Not Proceed by the Expected Aromatization Mechanism.”
205. Storici, P.; De Biase, D.; Bossa, F.; Bruno, S.; Mozzarelli, A.; Peneff, C.; Silverman, R. B.; Schirmer, T. J. Biol. Chem. 2004, 279, 363-373. “Structures of GABA Aminotransferase, a Pyridoxal 5′-Phosphate and [2Fe-2S] Cluster Containing Enzyme, Complexed with the Antiepilepsy Drug Vigabatrin and with γ-Ethynyl GABA.”
206. Gómez-Vidal, J. A.; Martásek, P.; Roman, L. J.; Silverman, R. B. J. Med. Chem. 2004, 47, 703-710. “Potent and Selective Conformationally-Restricted Neuronal Nitric Oxide Synthase Inhibitors.”
207. Wang, Z.; Silverman, R. B. J. Enz. Inhib. Med. Chem. 2004, 19, 293-301. “Synthesis of Cyclopropane Isosteres of the Antiepilepsy Drug Vigabatrin and Evaluation of their Inhibition of GABA Aminotransferase.”
208. Flinspach, M.; Li, H.; Jamal, J.; Yang, W.; Huang, H.; Silverman, R. B.; Poulos, T. L. Biochemistry 2004, 43, 5181-5187. “Structures of the Neuronal and Endothelial NOS Heme Domain with D-Nitroarginine-containing Dipeptide Inhibitors Bound.”
209. Schering, C. A.; Zhong, B.; Woo, J. C. G.; Silverman, R. B. Bioconj. Chem. 2004, 15, 673-676. “Poly(ethylene glycol)-Supported Enzyme Inactivators. Efficient Identification of the Site of Covalent Attachment to α-Chymotrypsin by PEG-TPCK.”
210. Pan, Y.; Calvert, K.; Silverman, R. B. Bioorg. Med. Chem. 2004, 12, 5719-5725. “Conformationally-Restricted Vigabatrin Analogues as Irreversible and Reversible Inhibiors of γ-Aminobutyric Acid Aminotransferase.”
211. Storici, P.; Qiu, J.; Schirmer, T.; Silverman, R. B. Biochemistry 2004, 43, 14057-14063. “Mechanistic Crystallography. Mechanism of Inactivation of γ-Aminobutyric Acid Aminotransferase by (1R,3S,4S)-3-Amino-4-fluorocyclopentane-1-carboxylic Acid as Elucidated by Crystallography.”
212. Westerheide, S. D.; Bosman, J. D.; Mbadugha, B. N. A.; Kawahara, T. L. A.; Matsumoto, G.; Gu, W.; Kim, S.; Devlin, J. P.; Silverman, R. B.; Morimoto, R. I. J. Biol. Chem. 2004, 279, 56053-56060. “Celastrols as Inducers of the Heat Shock Response and Cytoprotection.”
213. Zhu, Y.; Nikolic, D.; Van Breemen, R. B.; Silverman, R. B. J. Am. Chem. Soc. 2005, 127, 858-868. “Mechanism of Inactivation of Inducible Nitric Oxide Synthase by Amidines. Irreversible Enzyme Inactivation without Inactivator Modification.”
214. Erdal, E. P.; Litzinger, E. A.; Seo, J.; Zhu, Y.; Ji, H.; Silverman, R. B. Curr. Topics Med. Chem. 2005, 5, 603-624. “Selective Neuronal Nitric Oxide Synthase Inhibitors.”
215. Vintém, A. P. B.; Price, N. T.; Silverman, R. B.; Ramsay, R. R. Bioorg. Med. Chem. 2005, 13, 3487-3495. “Mutation of Surface Cysteine 374 to Alanine in Monoamine Oxidase A Alters Substrate Turnover and Inactivation by Cyclopropylamines.”
216. Liu, S.; Gu, W.; Lo, D.; Ding, X.-Z.; Ujiki, M.; Adrian, T. E.; Soff, G. A.; Silverman, R. B. J. Med. Chem. 2005, 48, 3630-3638. “N– Methylsansalvamide A Peptide Analogues. Potent New Antitumor Agents.”
217. Li, H.; Flinspach, M. L.; Igarashi, J.; Jamal, J.; Yang, W.; Gomez-Vidal, J. A.; Litzinger, E. A.; Huang, H.; Erdal, E. P.; Silverman, R. B.; Poulos, T. L. Biochemistry 2005, 44, 15222-15229. “Exploring the Binding Conformations of Bulkier Dipeptide Amide Inhibitors in Constitutive Nitric Oxide Synthases.”
218. Crittenden, D. L.; Park, A.; Qiu, J.; Silverman, R. B.; Duke, R. K.; Johnston, G. A. R.; Jordan, M. J. T.; Chebib, M. Bioorg. Med. Chem. 2006, 14, 447-455. “Enantiomers of cis-constrained and flexible 2-substituted GABA analogues exert opposite effects at recombinant GABAC receptors.”
219. Yuan, H.; Silverman, R. B. Bioorg. Med. Chem. 2006, 14, 1331-1338. “New Substrates and Inhibitors of γ-Aminobutyric Acid Aminotransferase Containing Bioisosteres of the Carboxylic Acid Group: Design, Synthesis, and Biological Activity.”
220. Ujiki, M. B.; Milam, B.; Ding, X.-Z.; Roginsky, A. B.; Salabat, M. R.; Talamonti, M. S.; Bell, R. H.; Gu, W.; Silverman, R. B.; Adrian, T. E. Biochem. Biophys. Res. Commun. 2006, 340, 1224-1228. “A Novel Peptide Sansalvamide A Analogue Inhibits Pancreatic Cancer Cell Growth Through G0/G1 Cell Cycle Arrest.”
221. Wang, Z.; Silverman, R. B. Biochemistry 2006, 14, 2242-2252. “Syntheses and Evaluation of Fluorinated Conformationally Restricted Analogues of GABA as Potential Inhibitors of GABA Aminotransferase.”
222. Litzinger, E. A.; Martásek, P.; Roman, L. J.; Silverman, R. B. Bioorg. Med. Chem. 2006, 14, 3185-3198. “Design, Synthesis, and Biological Testing of Potential Heme-Coordinating Nitric Oxide Synthase Inhibitors.”
223. Gu, W.; Nusinzon, I.; Smith, R. D. Jr.; Horvath, C. M.; Silverman, R. B. Bioorg. Med. Chem. 2006, 14, 3320-3329. “Carbonyl- and Sulfur-Containing Analogs of Suberoylanilide Hydroxamic Acid. Potent Inhibition of Histone Deacetylases.”
224. Mbadugha, B. N. A.; Seo, J.; Ji, H.; Martásek, P.; Roman, L. J.; Shea, T. M.; Silverman, R. B. Bioorg. Med. Chem.2006, 14, 3681-3690. “Hydroxyl-terminated Peptidomimetic Inhibitors of Neuronal Nitric Oxide Synthase.”
225. Seo, J.; Silverman, R. B. Tetrahedron Lett., 2006, 47, 4069-4073. “Synthesis of Arginine-containing Hydroxamate Dipeptidomimetics.”
226. Lawton, G. L.; Ji, H.; Silverman, R. B. Tetrahedron Lett., 2006, 47, 6113-6115. “Remote Protection Prevents Unwanted Cyclizations with 2-Aminopyridines.”
227. Ji, H.; Gómez-Vidal, J. A.; Martásek, P.; J. Roman, L. J.; Silverman, R. B. J. Med. Chem., 2006, 49, 6254-6263. “Conformationally-Restricted Dipeptide Amides as Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors.”
228. Lu, H.; Silverman, R. B. J. Med. Chem., 2006, 49, 7404-7412. “Fluorinated Conformationally-Restricted γ-Aminobutyric Acid Aminotransferase Inhibitors.”
229. Wang, Z.; Yuan, H.; Silverman, R. B. Biochemistry, 2006, 45, 14513-14522. “(±)-(1S,2R,5S)-5-Amino-2-fluorocyclohex-3-ene Carboxylic Acid, A Potent GABA Aminotransferase Inactivator that Irreversibly Inhibits through an Elimination-Aromatization Pathway.”
230. Zhu, Y.; Silverman, R. B. J. Org. Chem., 2007, 72, 233-239. “Electronic Effects of Peripheral Substituents on Porphyrin Meso-Positions.”
231. Seo, J.; Igarashi, J.; Li, H.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. J. Med. Chem. 2007, 50, 2089-2099. “Structure-Based Design and Synthesis of Nw-Nitro-L-Arginine-Containing Peptidomimetics as Selective Inhibitors of Neuronal Nitric Oxide Synthase. Displacement of the Heme Structural Water.”
232. Seo, J.; Martásek, P.; Roman, L. J.; Silverman, R. B. Bioorg. Med. Chem. 2007, 15, 1928-1938. “Selective L-Nitroargininylaminopyrrolidine and L-Nitroargininylaminopiperidine Neuronal Nitric Oxide Synthase Inhibitors.”
233. Yuan, H.; Silverman, R. B. Bioorg. Med. Chem. Lett. 2007, 17, 1651-1654.”Structural Modifications of (1S,3S)-3-Amino-4-Difluoromethylenecyclopentanecarboxylic Acid, a Potent Irreversible Inhibitor of GABA Aminotransferase.”
234. Zhu, Y.; Silverman, R. B. Org. Lett. 2007, 9, 1195-1198. “Model Studies for Heme Oxygenase-Catalyzed Porphyrin Meso Hydroxylation.”
235. Gu, W.; Cueto, M.; Jensen, P. R.; Fenical, W.; Silverman, R. B. Tetrahedron 2007, 63, 6535-6541. “Microsporins A and B: new histone deacetylase inhibitors from the marine-derived fungus Microsporum cf. gypseum and the solid-phase synthesis of microsporin A.”
236. Erdal, E. P.; Martásek, P.; Linda J. Roman, L. J.; Silverman, R. B. Bioorg. Med. Chem. 2007, 15, 6096-6108. “Hydroxyethylene Isosteres of Selective Neuronal Nitric Oxide Synthase Inhibitors.”
237. Clift, M.; Ji, H.; Deniau, G. P.; O’Hagan, D.; Silverman, R. B. Biochemistry 2007, 46(48), 13819-13828. “The Enantiomers of 4-Amino-3-fluorobutanoic Acid as Substrates for g-Aminobutyric Acid Aminotransferase. Conformational Probes for GABA Binding.”
238. Liu, D.; Pozharski, E.; Lepore, B. W.; Fu, M.; Silverman, R. B.; Petsko, G. A.; Ringe, D. Inactivation of Escherichia coli L-Aspartate Aminotransferase by (S)-4-Amino-4,5-dihydro-2-thiophenecarboxylic Acid Reveals A Tale of Two Mechanisms. Biochemistry 2007, 46(37), 10517-10527.
239. Silverman, R. B. Angew. Chem. Int. Ed. 2008, 47, 3500-3504. “From Basic Science to Blockbuster Drug. The Discovery of Lyrica.”
240. Clift, M. D.; Silverman, R. B. Bioorg. Med. Chem. Lett. 2008, 18 (10), 3122-3125. “Synthesis and Evaluation of Novel Aromatic Substrates and Competitive Inhibitors of GABA Aminotransferase.”
241. Ji, H.; Stanton, B. Z.; Igarashi, J.;, Li, H.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. J. Am. Chem. Soc. 2008, 130(12), 3900-3914. “Minimal Pharmacophoric Elements and Fragment Hopping, an Approach Directed at Molecular Diversity and Isozyme Selectivity. Design of Selective Neuronal Nitric Oxide Synthase Inhibitors.”
242. Zhu, Y.; Silverman, R. B. Biochemistry 2008, 47(8), 2231-2243. “Revisiting Heme Mechanisms. A Perspective on the Mechanisms of Nitric Oxide Synthase (NOS), Heme Oxygenase (HO), and Cytochrome P450s (CYP450s).”
243. Trott, A.; West, J. D.; Klaic, L.; Westerheide, S. D.; Silverman, R. B.; Morimoto, R. I.; Morano, K. A. Mol. Biol. Cell 2008, 19(3), 1104-1112. “Activation of Heat Shock and Antioxidant Responses by the Natural Product Celastrol: Transcriptional Signatures of a Thiol-targeted Molecule.”
244. Silverman, R. B., Enzyme Inhibition In Wiley Encyclopedia of Chemical Biology; John Wiley & Sons, Hoboken, 2009, Volume 1, pp 663-681.
245. Ji,H.; Tan,S.; Igarashi,J.; Li,H.; Derrick,M.; Martásek,P.; Roman,L. J.; Vásquez-Vivar,J.; Poulos,T. L.; Silverman, R. B. Ann. Neurol. 2009, 65, 209-217. “Selective Neuronal Nitric Oxide Synthase Inhibitors for Prevention of Cerebral Palsy.”
246. Ji, H.; Erdal, E. P.; Litzinger, E. A.; Seo, J.; Zhu, Y.; Xue, F.; Fang, J.; Huang, J.; Silverman, R. B. Frontiers in Medicinal Chemistry, Reitz, A. B.; Choudhary, M. I.; Atta-ur-Rahman, Editors; Bentham Science Publishers, Volume 5, 2009, 842-882. “Selective Neuronal Nitric Oxide Synthase Inhibitors.”
247. Ji,H.; Li, H.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. J. Med. Chem. 2009, 52 (3), 779–797. ” Discovery of Highly Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase by Fragment Hopping.”
248. Silverman, R. B. Acc. Chem. Res. 2009, 42, 439-451. ” Design of Selective Neuronal Nitric Oxide Synthase Inhibitors for the Prevention and Treatment of Neurodegenerative Diseases.”
249. Igarashi, J.; Li, H.; Jamal, J.; Ji, H.; Fang, J.; Lawton, G. R.; Silverman, R. B.; Poulos, T. L. J. Med. Chem. 2009, 52, 2060-2066. “Crystal Structures of Constitutive Nitric Oxide Synthases in Complex with De Novo Designed Inhibitors.”
250. Lawton, G. R.;Ralay Ranaivo, H.; Wing, L. K.; Ji, H.; Xue, F.; Martásek, P.; Roman, L. J.; Watterson, D. M.; Silverman, R. B. Bioorg. Med. Chem. 2009, 17(6), 2371-2380. ” Analogues of 2-aminopyridine-based Selective Inhibitors of Neuronal Nitric Oxide Synthase with Increased Bioavailability.”
251. Fang, J.; Ji,H.; Lawton, G. R.; Xue, F.; Martásek, P.; Roman, L. J.; Silverman, R. B. J. Med. Chem. 2009, 52, 4533-4537. “L337H Mutant of Rat Neuronal Nitric Oxide Synthase Resembles Human Neuronal Nitric Oxide Synthase Toward Inhibitors.”
252. Fang, J.; Silverman, R. B. Anal. Biochem. 2009, 390, 74-78. “A Cellular Model for Screening Neuronal Nitric Oxide Synthase Inhibitors.”
253. Lawton, G. R.; Ji,H.; Martásek, P.; Roman, L. J.; Silverman, R. B. Beilstein J. Org. Chem. 2009, 5, No. 28. “Synthesis and Enzymatic Evaluation of 2- and 4-aminothiazole-based Inhibitors of Neuronal Nitric Oxide Synthase.”
254. Derrick, M.; Drobyshevsky, A.; Ji, X.; Chen, L.; Yang, Y.; Ji, H.; Silverman, R. B.; Tan, S. Hypoxia-ischemia causes persistent movement deficits in a perinatal rabbit model of cerebral palsy: assessed by a new swim test. Int. J. Devel. Neurosci. 2009, 27(6), 549-557. PMCID: PMC2728796
255. Silverman, R. B.; Lawton, G. R.; Ralay Ranaivo, H.; Seo, J.; Watterson, D. M. Effect of Potential Amine Prodrugs of Selective Neuronal Nitric Oxide Synthase Inhibitors on Blood-Brain Barrier Penetration. Bioorg. Med. Chem. 2009, 17, 7593-7605.
256. Xue, F.; Gu, W.; Silverman, R. B. A Concise Route to the Chiral Pyrrolidine Core for Inhibitors of Neuronal Nitric Oxide Synthase. Org. Lett. 2009, 11 (22), 5194–5197.
257. Delker, D. L.; Ji, H.; Li, H.; Jamal, J.; Fang, J.; Xue, X.; Silverman, R. B.; Poulos, T. L. Unexpected Binding Modes of Nitric Oxide Synthase Inhibitors Effective in the Prevention of Cerebral Palsy, J. Am. Chem. Soc. 2010, 132, 5437–5442.
258. Martell, J. D.; Li, H.; Doukov, T.; Martásek, P.; Roman, L. J.; Soltis, M.; Poulos, T. L.; Silverman, R. B. Heme-Coordinating Inhibitors of Neuronal Nitric Oxide Synthase. Iron-Thioether Coordination is Stabilized by Hydrophobic Contacts Without Increased Inhibitor Potency. J. Am. Chem. Soc. 2010, 132(2), 798–806.
259. Kudoh, T.; Park, C. S.; Lefurgy, S. T.; Sun, M.; Michels, T.; Leyh, T. S.; Silverman, R. B. Mevalonate Analogues as Substrates of Enzymes in the Isoprenoid Biosynthetic Pathway of Streptococcus pneumoniae. Bioorg. Med. Chem. 2010, 18, 1124-1134.
260. Xue, F.; Fang, J.; Lewis, W. W.; Martásek, P.; Roman, L. J.; Silverman, R. B. Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability. Bioorg. Med. Chem. Lett. 2010, 20, 554-557.
261. Heiferman, M. J.; Salabat, M. R.; Ujiki, M. B.; Strouch, M. J.; Cheon, E. C.; Silverman, R. B.; Bentrim, D. J. Sansalvamide induces pancreatic cancer growth arrest through changes in the cell cycle. Anticancer Res. 2010, 30, 73.
262. Xue, F.; Silverman, R. B. An Alkoxide Anion Triggered tert-Butyloxycarbonyl Group Migration. Mechanism and Application. Tetrahedron Lett. 2010, 51, 2536-2538.
263. Chang, C.-C.; Cao, S.; Kang, S.; Kai, L.; Tian, X.; Pandey, P.; Fernandez Dunne, S.; Luan, C.-H.; Surmeier, D. J.; Silverman, R. B. Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels CaV1.3 and CaV1.2. Bioorg. Med. Chem 2010, 18, 3147-3158.
264. Lepore, B. W.; Liu, D.; Peng, Y.; Fu, M.; Yasuda, C.; Manning, J. M.; Silverman, R. B.; Ringe, D. Chiral discrimination among aminotransferases: inactivation by 4-amino-4,5-dihydrothiophenecarboxylic acid. Biochemistry 2010 49(14), 3138-47.
265. Lefurgy, S. T.; Rodriguez, S. B.; Park, C. S.; Cahill, S.; Silverman, R. B.; Leyh, T. S. Probing ligand-binding pockets of the mevalonate pathway enzymes from Streptococcus pneumoniae. J Biol. Chem. 2010, 285(27), 20654-63.
266. Xue, F.; Huang, J.; Ji, H.; Li, H.; Martasek, P.; Roman, L. J.; Poulos, T. P.; Silverman, R. B. Structure-based design, synthesis, and biological evaluation of lipophlic-tailed monocationic inhibitors of neuronal nitric oxide synthase. Bioorg. Med. Chem. 2010, 18, 6526-6261.
267. Xue, F.; Li, H.; Fang, J.; Roman, L. J.; Martasek, P.; Poulos T.L.; Silverman, R. B. Peripheral but crucial: a hydrophobic pocket (Tyr706, Leu337, and Met336) for potent and selective inhibition of neuronal nitric oxide synthase. Bioorg. Med. Chem. Lett. 2010, 20, 6258-6261.
268. Xue, F.; Li, H.; Delker, S.; Fang, J.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Potent, Highly Selective, and Orally Bioavailable Gem-Difluorinated Monocationic Inhibitors of Neuronal Nitric Oxide Synthase, J. Am. Chem. Soc. 2010, 132(40), 14229-14238.
269. Ji, H.; Delker, S. L.; Li, H.; Martásek, P.; Roman, L. J.; Poulos, T.P.; Silverman, R. B. Exploration of the active site of neuronal nitric oxide synthase by the design and synthesis of pyrrolidinomethyl 2-aminopyridine derivatives. J. Med. Chem. 2010, 53, 7804-7824.
270. Delker, S. L.; Xue, F.; Li, H.; Jamal, J.; Silverman, R. B.; Poulos, T.P. Role of zinc in isoform selective inhibitors of neuronal nitric oxide synthase. Biochemistry 2010, 49, 10803-10810.
271. Liu, D.; Pozharski, E.; Fu, M.; Silverman, R. B.; Ringe, D. Mechanism of Inactivation of Escherichia coli Aspartate Aminotransferase by (S)-4-Amino-4,5-dihydro-2-furancarboxylic Acid. Biochemistry 2010, 49(49), 10507-10515.
272. Chen, T.; Benmohamed, R.; Arvanites, A. C.; Ranaivo, H. R.; Morimoto, R. I.; Ferrante, R. J.; Watterson, D. M.; Kirsch, D. R.; Silverman, R. B. Arylsulfanyl Pyrazolones Block Mutant SOD1-G93A Aggregation. Potential Application for the Treatment of Amyotrophic Lateral Sclerosis. Bioorg. Med. Chem. 2010, 19, 613-622.
273. Yu, L.; Derrick, M.; Ji, H.; Silverman, R. B.; Whitsett, J.; Vasquez-Vivar, J.; Tan, S. Neuronal nitric oxide synthase inhibition prevents cerebral palsy following hypoxia-ischemia in fetal rabbits: Comparison between JI-8 and 7-nitroindazole. Dev. Neurosci. 2011, 33, 312-319.
274. Benmohamed, R.; Arvanites, A. C.; Kim, J.; Ferrante, R. J.; Silverman, R. B.; Morimoto, R. I.; Kirsch, D. R. Identification of compounds protective against G93A SOD1 toxicity for the treatment of amyotrophic lateral sclerosis. Amyotroph. Lat. Scler. 2011, 12, 87-96.
275. Xue, F.; Delker, S. L.; Li, H.; Fang, J.; Martásek, P.; Roman, L. J.; Poulos, T.P.; Silverman, R. B. Symmetric double-headed aminopyridines. A novel strategy for potent and membrane-permeable inhibitors of neuronal nitric oxide synthase. J. Med. Chem. 2011, 54, 2039-2048.
276. Rao, S.; Lin, Z.; Drobyshevsky, A.; Chen, L.; Ji, X.; Ji, H.; Yang, Y.; Yu, L.; Derrick, M.; Silverman, R. B.; Tan, S. Involvement of Neuronal Nitric Oxide Synthase in Ongoing Fetal Brain Injury Following Near-Term Rabbit Hypoxia-Ischemia. Dev. Neurosci. 2011, 33, 288-298.
277. Xia, G.; Benmohamed, R.; Kim, J.; Arvanites, A. C.; Morimoto, R. I.; Ferrante, R. J.; Kirsch, D. R.; Silverman, R. B. Pyrimidine-2,4,6-trione Derivatives and Their Inhibition of Mutant SOD1-dependent Protein Aggregation. Toward a Treatment for Amyotrophic Lateral Sclerosis (ALS). J. Med. Chem. 2011, 54, 2409-2421.
278. Doukov, T.; Li, H.; Sharma, A.; Martell, J. D.; Soltis, M.; Silverman, R. B.; Poulos, T. L.; Temperature dependent spin crossover in neuronal nitric oxide synthase bound with the heme-coordinating thioether inhibitors. J. Am. Chem. Soc. 2011, 133, 8326-8334.
279. Xue, F.; Kraus, J. M.; Jansen Labby, K.; Ji, H.; Mataka, J.; Xia, G.; Li, H.; Delker, S. L.; Roman, L. J.; Martásek, P.; Poulos, T. L.; Silverman, R. B. Improved Synthesis of Chiral Pyrrolidine Inhibitors and Their Binding Properties to Neuronal Nitric Oxide Synthase. J. Med. Chem. 2011, 54, 6399-6403.
280. Gu, W.; Silverman, R. B. Synthesis of (S)-2-Boc-Amino-8-(R)-(tert-butyldimethylsilanyloxy)decanoic acid, a Precursor to the Unusual Amino Acid Residue of the Anticancer Agent Microsporin B Tetrahedron Lett. 2011, 52, 5438-5440.
281. Gu, W.; Silverman, R. B. Stereospecific Total Syntheses of Proteasome Inhibitors Omuralide and Lactacystin. J. Org. Chem. 2011, 76, 8287-8293.
282. Watanabe, M.; Yamaguchi, K.; Tang, W.; Yoshida, K.; Silverman, R. B.; Arisawa, M.; Shuto, S. Synthesis of a series of 3,4-methanoarginines as side-chain conformationally-restricted analogues of arginine. Bioorg. Med. Chem. 2011, 19, 5984-5988.
283. Klaic, L.; Trippier, P.; Mishra, R.; Morimoto, R. I.; Silverman, R. B. Remarkable stereospecific conjugate additions to the Hsp90 inhibitor celastrol. J. Am. Chem. Soc., 2011, 133(49), 19634-19637.
284. Pan, Y.; Gerasimov, M. R.; Kvist, T.; Wellendorph, P.; Madsen, K. K.; Pera, E.; Lee, H.; Schousboe, A.; Chebib, M.; Bräuner-Osborne, H.; Craft, C. M.; Brodie, J. D.; Schiffer, W. K.; Dewey, S. L.; Miller, S. R.; Silverman, R. B. CPP-115, a Potent g-Aminobutyric Acid Aminotransferase Inactivator for the Treatment of Cocaine Addiction. J. Med. Chem. 2012, 55, 357-366.
285. Zhang, W.; Benmohamed, R.; Arvanites, A. C.; Morimoto, R. I.; Ferrante, R. J.; Kirsch, D. R.; Silverman, R. B. Cyclohexane 1,3-diones and their inhibition of mutant SOD1-dependent protein aggregation and toxicity in PC12 cells. Bioorg. Med. Chem. 2012, 20, 1029-1045.
286. Ji, H.; Jing, Q.; Huang, J.; Silverman, R. B. Acid-Facilitated Debenzylation of N-Boc, N-Benzyl Double Protected 2-Aminopyridinomethylpyrrolidine Derivatives. Tetrahedron 2012, 68, 1359-1366.
287. Chen, T.; Benmohamed, R.; Kim, J.; Smith, K.; Amante, D.; Morimoto, R. I.; Kirsch, D. R.; Ferrante, R. J.; Silverman, R. B. ADME-Guided Design and Synthesis of Aryloxanyl Pyrazolone Derivatives to Block Mutant SOD1 Cytotoxicity and Protein Aggregation: Potential Application for the Treatment of Amyotrophic Lateral Sclerosis. J. Med. Chem. 2012, 55, 515-527.
288. Kraus, J. M.; Gits, H.; Silverman, R. B. High yielding allylation of a chiral secondary alcohol containing base sensitive functional groups. Tetrahedron Lett. 2012 53, 1319-1322.
289. Silverman, R. B. The 2011 E. B. Hershberg Award for Important Discoveries in Medicinally Active Substances: (1S,3S)-3-Amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a GABA Aminotransferase Inactivator and New Treatment for Drug Addiction and Infantile Spasms. J. Med. Chem. 2012, 55, 567-575.
290. Jansen Labby, K.; Xue, F.; Kraus, J. M.; Ji, H.; Mataka, J.; Li, H.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Intramolecular Hydrogen Bonding: A Potential Strategy for More Bioavailable Inhibitors of Neuronal Nitric Oxide Synthase, Bioorg. Med. Chem. 2012, 20, 2435-2443.
291. Choi, S. H.; Quinti, L.; Kazantsev, A. G.; Silverman, R. B. 3-(N-Arylsulfamoyl)benzamides, Inhibitors of Human Sirtuin Type 2 (SIRT2). Bioorg. Med. Chem. Lett. 2012, 22, 2789-2793.
292. Klaic, L.; Morimoto, R. I.; Silverman, R. B. Celastrol Analogs as Inducers of the Heat Shock Response. Design and Synthesis of Affinity Probes for the Identification of Protein Targets. ACS Chem. Biol. 2012, 7, 928-937.
293. Zhang, Y.; Silverman, R. B. Direct amination of gamma-halo-beta-ketoesters with anilines. J. Org. Chem. 2012, 77, 3462-3467.
294. Huang, H.; Ji, H.; Li, H.; Jing, Q.; Jansen Labby, K.; Martásek, P.; Roman, L. J.; Poulos, T. P.; Silverman, R. B. Selective Monocationic Inhibitors of Neuronal Nitric Oxide Synthase. Binding Mode Insights from Molecular Dynamics Simulations. J. Am. Chem. Soc. 2012, 134, 11559-11572.
295. Zhang, Y.; Benmohamed, R.; Zhang, W.; Kim, J.; Edgerly, C.; Zhu, Y.; Morimoto, R. I.; Ferrante, R. J.; Kirsch, D. R.; Silverman, R. B. Chiral cyclohexane 1,3-diones as inhibitors of mutant SOD1-dependent protein aggregation for the treatment of ALS. ACS Med. Chem. Lett. 2012, 3, 584-587.
296. Kang, S.; Cooper, G.; Dunne, S. F.; Dusel, B.; Luan, C.-H.; Surmeier, D. J.; Silverman, R. B. CaV1.3-selective L-type calcium channel antagonists as potential new therapeutics for Parkinson’s disease. Nature Commun. 2012, 3, 1146.
297. Drobyshevsky, A.; Yu, L.; Yang, Y.; Khalid, S.; Luo, K.; Jiang, R.; Ji, H.; Derrick, M.; Kay, L.; Silverman, R. B.; Tan, S.Antenatal Insults Modify Newborn Olfactory Function By Nitric Oxide Produced From Neuronal Nitric Oxide Synthase. Exp. Neurol. 2012, 237, 427-434.
298. Trippier, P.; Benmohamed, R.; Kirsch, D. R.; Silverman, R. B. Substituted pyrazolones require N2 hydrogen bond donating ability to protect against cytotoxicity from protein aggregation of mutant super-oxide dismutase 1. Bioorg. Med. Chem. Lett. 2012, 22, 6647-6650.
299. Hawker, D. D.; Silverman, R. B. Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase. Bioorg. Med. Chem. 2012, 20, 5763-5773.
300. Yang, Z.; Misner, B.; Ji, H.; Poulos, T. L.; Silverman, R. B.; Meyskens, F. L.; Yang, S. Targeting nitric oxide (NO) signaling as a novel strategy for the therapy and prevention of human melanoma. Antioxid. Redox Signal. 2013, 1-15.
301. Chopra, V.; Quinti, L.; Kim, J.; Vollor, L.; Kumaraswamy. L.; Edgerly, C.; Cipicchio, P. M.; Lauver, M. A.; Choi, S. H.; Sittampalli, B.; Silverman, R. B.; Ferrante, R. J.; Steven Hersch, S.; Kazantsev, A. G. The Sirtuin 2 Inhibitor AK-7 is Neuroprotective in Huntington Disease Mouse Models, Cell Rep. 2012, 2, 1492-7.
302. Jansen Labby, K.; Li, H.; Martasek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Methylated Nw-hydroxy-L-arginine analogues as mechanistic probes for the second step of the nitric oxide synthase-catalyzed reaction. Biochemistry 2013, 52, 3062-3073.
303. Zhang, Y.; Silverman, R. B. A novel synthesis of 1-aryl-3-piperidone derivatives. Tetrahedron Lett. 2013, 54, 573-575.
304. Juncosa, Jr., J. I.; Groves, A. P.; Xia, G.; Silverman, R. B. Probing the steric requirements of the g-aminobutyric acid aminotransferase active site with fluorinated analogues of vigabatrin. Bioorg. Med. Chem. 2013, 21, 903-911.
305. Huang, H.; Silverman, R. B. Recent Advances Toward Improving the Bioavailability of Neuronal Nitric Oxide Synthase Inhibitors. Curr. Top. Med. Chem. 2013, 13, 803-812.
306. Li, H.; Xue, F.; Kraus II, J. M.; Ji, H.; Jansen Labby, K.; Mataka, J.; Delker, S. L.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase. Bioorg. Med. Chem. 2013, 21, 1333-1343.
307. Trippier, P. C.; Jansen Labby, K.; Hawker, D. D.; Mataka, J. J.; Silverman, R. B. Target- and mechanism-based therapeutics for neurodegenerative diseases: strength in numbers. J. Med. Chem., 2013, 56, 3121-3147.
308. Zhang, Y.; Benmohamed, R.; Huang, H.; Chen, T.; Voisine, C.; Morimoto, R. I.; Kirsch, D. R.; Silverman, R. B. Arylazanylpyrazolone derivatives as inhibitors of mutant SOD1-dependent protein aggregation for the treatment of amyotrophic lateral sclerosis, J. Med. Chem. 2013, 56, 2665-2675.
309. Huang, H.; Li, H.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Structure-guided design of selective inhibitors of neuronal nitric oxide synthase, J. Med. Chem. 2013, 56, 3024-3032.
310. Kang, S.; Cooper, G.; Dunne, S. F.; Luan, C.-H.; Surmeier, D. J.; Silverman, R. B. Antagonism of L-type Ca2+channels CaV1.3 and CaV1.2 by 1,4-dihydropyrimidines and 4H-pyrans as dihydropyridine mimics. Bioorg. Med. Chem. 2013, 21, 4365-4373.
311. Kang, S.; Cooper, G.; Dunne, S. F.; Luan, C.-H.; Surmeier, D. J.; Silverman, R. B. Structure-activity relationship of N,N’-disubstituted pyrimidinetriones as CaV1.3 channel-selective antagonists for Parkinson’s disease. J. Med. Chem. 2013, 56, 4786-4797.
312. Juncosa, J. I.; Lee, H.; Silverman, R. B. Two continuous coupled assays for ornithine-d-aminotransferase. Anal. Biochem. 2013, 440, 145-149.
313. Jing, Q.; Li, H.; Fang, J.; Roman, L. J.; Martásek, P.; Poulos, T. L.; Silverman, R. B. In search of potent and selective inhibitors of neuronal nitric oxide synthase with more simple structures. Bioorg. Med. Chem. 2013, 21, 5323-5331.
314. Huang, H.; Li, H.; Yang, S.; Chreifi, G.; Martásek, P.; Roman, L. J.; Meyskens, F. L.; Poulos, T. L.; Silverman, R. B. Potent and Selective Double-headed Thiophene-2-carboximidamide Inhibitors of Neuronal Nitric Oxide Synthase for the Treatment of Melanoma. J. Med. Chem. 2014, 57, 686-700.
315. Jing, Q.; Li, H.; Chreifi, G.; Roman, L. J.; Martásek, P.; Poulos, T. L.; Silverman, R. B. Chiral linkers to improve selectivity of double-headed neuronal nitric oxide synthase inhibitors. Bioorg. Med. Chem. Lett. 2013, 23, 5674-5679.
316. Holden, J. K.; Li, H.; Jing, Q.; Kang, S.; Richo, J.; Silverman, R. B.; Poulos, T. L. Structural and biological studies on bacterial nitric oxide synthase inhibitors. Proc. Natl. Acad. Sci. U.S.A. 2013, 110, 18127-18131.
317. Walia, A.; Kang, S.; Silverman, R. B. Microwave-assisted protection of primary amines as 2,5-dimethylpyrroles and their orthogonal deprotection. J. Org. Chem. 2013, 78, 10931-10937.
318. Drury, P. P.; Davidson, J. O.; van Den Heuij, L.; Tan, S.; Silverman, R. B.; Ji, H.; Blood, A.; Fraser, M.; Bennet, L.; Gunn, A. J. Partial neuroprotection by nNOS inhibition during profound asphyxia in preterm fetal sheep. Exp. Neurol. 2013, 250, 282-292.
319. Jing, Q.; Li, H.; Roman, L. J.; Martásek, P.; Poulos, T. L.; Silverman, R. B. An accessible chiral linker to enhance potency and selectivity of neuronal nitric oxide synthase inhibitors. ACS Med Chem Lett 2014, 5, 56-60.
320. Mukherjee, P.; Cinelli, M. A.; Kang, S.; Silverman, R. B. Development of nitric oxide synthase inhibitors for neurodegeneration and neuropathic pain. Chem. Soc. Rev. 2014, Chem. Soc. Rev. 2014, 43(19), 6814-6838. PMCID: PMC4138306
321. Khanfar, M. A.; Quinti, L.; Wang, H.; Choi, S. H.; Kazantsev, A. G.; Silverman, R. B. Development and characterization of 3-(benzylthio)benzamides as potent and selective SIRT2 inhibitors. Eur. J. Med. Chem. 2014, 76, 414-426.
322. Cinelli, M. A.; Li, H.; Chriefi, G.; Martasek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Simplified 2-aminoquinoline-based scaffold for potent and selective neuronal nitric oxide synthase inhibition. J. Med. Chem. 2014, 57(4), 1513-1530.
323. Drury, P. P; Davidson, J. O.; van den Heuij, L G.; Bennet, L.; Tan, S.; Silverman, R. B.; Ji, H.; Gunn, A. J. nNOS inhibition during profound asphyxia reduces seizure burden and improves survival of striatal phenotypic neurons in preterm fetal sheep. Neuropharmacol. 2014, 83, 62-70.
324. Kang, S.; Tang, W.; Li, H.; Chreifi, G.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Nitric oxide synthase inhibitors that interact with both a heme propionate and tetrahydrobiopterin show high isoform selectivity. J. Med. Chem. 2014, 57 (10), pp. 4382-4396.
325. Trippier, P. C.; Zhao, K. T.; Fox, S. G.; Schiefer, I. T.; Benmohamed, R.; Moran, J.; Kirsch, D. R.; Morimoto, R. I.; Silverman, R. B. Proteasome Activation is a Mechanism for Pyrazolone Small Molecules Displaying Therapeutic Potential in Amyotrophic Lateral Sclerosis. ACS Chem. Neurosci. 2014, 5, 823-829. PMCID: PMC4176317
326. Lee, H.; Juncosa, J. I.; Silverman, R. B. Ornithine aminotransferase vs. GABA aminotransferase. Implications for the design of new anticancer drugs. Med. Res. Rev. 2015, 35, 286-305. PMCID: PMC4415689
327. Davydov, R.; Jansen Labby, K.; Chobot, S. E.; Lukoyanov, D. A.; Crane, B. R.; Silverman, R. B.; Hoffman, B. M. Enzymatic and cryoreduction EPR studies of the hydroxylation of methylated Nw-hydroxy-L-arginine analogues by nitric oxide synthase from Geobacillus stearothermophilus. Biochemistry, 2014, 53 (41), 6511-6519. PMCID: PMC4204881
328. Li, H.; Jamal, J.; Plaza, C.; Pineda, S. H.; Chreifi, G.; Jing, Q.; Cinelli, M. A.; Silverman, R. B.; Poulos, T. L. Structures of human constitutive nitric oxide synthases. Acta Crystallog. D, 2014, D70, 2667-2674. PMCID: PMC4188008
329. Jing, Q.; Li, H.; Roman, L. J.; Martásek, P.; Poulos, T. L.; Silverman, R. B. Combination of chiral linkers with thiophenecarboximidamide heads to improve the selectivity of inhibitors of neuronal nitric oxide synthase. Bioorg. Med. Chem. Lett. 2014, 24, 4504-4510. PMCID: PMC4204799
330. Li, H.; Jamal, J.; Delker, S.; Ji, H.; Jing, Q.; Huang, H.; Kang, S.; Silverman, R. B.; Poulos, T. L. The mobility of a conserved tyrosine residue controls isoform-dependent enzyme-inhibitor interactions in nitric oxide synthases. Biochemistry, 2014, 53, 5272-5279. PMCID: PMC4139154
331. Kang, S.; Watanabe, M.; Jacobs, J.C.; Yamaguchi, M.; Dahesh, S.; Nizet, V.; Leyh, T. S.; Silverman, R. B. Synthesis of mevalonate- and fluorinated mevalonate prodrugs and their in vitro human plasma stability. Eur. J. Med. Chem. 2015, 90, 448-461. PMCID: PMC4291291
332. Chen, X.; Wales, P.; Quinti, L.; Moniot, S.; Herisson, F.; Abdul Rauf, N.; Zuo, F.; Wang, H.; Silverman, R. B.; Ayata, C.; Maxwell, M. M.; Clemens, S.; Schwarzschild, M. A.; Outeiro, T. F.; Kazantsev, A. G. The sirtuin-2 inhibitor AK7 is neuroprotective in models of Parkinson’s disease but not amyotrophic lateral sclerosis and cerebral ischemia. PLOS ONE2015, 10(1):e0116919. doi: 10.1371/journal.pone.0116919. PMCID: PMC4301865
333. Özdinler, P. H.; Silverman, R. B. Treatment of amyotrophic lateral sclerosis: Lessons learned from many failures. ACS Med. Chem. Lett. 2015, 5 (11), 1179-1181. PMCID: PMC4233364
334. Xia, G.; Benmohamed, R.; Morimoto, R. I.; Kirsch, D. R.; Silverman, R. B. Deuteration and fluorination of 1,3-bis(2-phenylethyl)pyrimidine-2,4,6(1H,3H,5H)-trione to improve its pharmacokinetic properties. Bioorg. Med. Chem. Lett. 2014, 24, 5098-5101. PMCID: PMC4250310
335. Mukherjee, P.; Li, H.; Sevrioukova, I.; Chreifi, G.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase. J. Med. Chem. 2015, 58, 1067–1088. (Editor’s Choice; cover art) PMCID: PMC4329833
336. Holden, J. K.; Kang, S.; Hollingsworth, S. A.; Li, H.; Lim, N.; Chen, S.; Huang, H.; Xue, F.; Tang, W.; Silverman, R. B.; Poulos, T. L. Structure-based design of bacterial nitric oxide synthase inhibitors. J. Med. Chem. 2015, 58, 994-1004. PMCID: PMC4306518
337. Lee, H.; Doud, E. H.; Wu, R.; Sanishvili, R.; Juncosa, J. I.; Liu, D.; Kelleher, N. L.; Silverman, R. B. Mechanism of inactivation of g-aminobutyric acid aminotransferase by (1S,3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115). J. Am. Chem. Soc. 2015, 137, 2628-240. PMCID: PMC4353033
338. Le, H. V.; Hawker, D. D.; Wu, R.; Doud, E.; Widom, J.; Sanishvili, R.; Liu, D.; Kelleher, N. L.; Silverman, R. B. Design and mechanism of tetrahydrothiophene-based GABA aminotransferase inactivators. J. Am. Chem. Soc. 2015, 137, 4525-4533. PMCID: PMC4390550
339. Tang, W.; Li, H.; Doud, E. H.; Chen, Y.; Choing, S.; Plaza, C.; Kelleher, N. L.; Poulos, T. L.; Silverman, R. B. Mechanism of inactivation of neuronal nitric oxide synthase by (S)-2-amino-5-(2-(methylthio)acetimidamido)pentanoic acid. J. Am. Chem. Soc. 2015, 137, 5980-5989. PMCID: PMC4431946
340. Tang, W.; Li, H.; Poulos, T. L.; Silverman, R. B. Mechanistic Studies of Inactivation of Inducible Nitric Oxide Synthase by Amidines. Biochemistry 2015, 54, 2530-2538. Highlighted on the journal home page. PMCID: PMC4410366
341. Khanfar, M. A.; Quinti, L.; Wang, H.; Nobles, J.; Kazantsev, A. G.; Silverman, R. B. Design and evaluation of 3-(benzylthio)benzamide derivatives as potent and selective SIT2 inhibitors. ACS Med. Chem. Lett. 2015, 6, 607-611. PMCID: PMC4434462
342. Lee, H.; Le, H. V.; Wu, R.; Doud, E.; Sanishvili, R.; Kellie, J. F.; Compton, P. D.; Pachaiyappan, B.; Liu, D.; Kelleher, N. L.; Silverman, R. B. Mechanism of inactivation of GABA aminotransferase by (E)- and (Z)-(1S,3S)-3-amino-4-fluoromethylenyl-1-cyclopentanoic acid. ACS Chem. Biol. 2015, 2087-2098. PMCID: PMC4575653
343. Zigmond, E.; Ya’acov, A. B.; Lee, H.; Lichtenstein, Y.; Shalev, Z.; Smith, Y.; Zolotarov, L.; Ziv, E.; Kalman, R.; Le, H. V.; Lu, H.; Silverman, R. B.; Ilan, Y. Suppression of hepatocellular carcinoma by inhibition of overexpressed ornithine aminotransferase. ACS Med. Chem. Lett. 2015, 6, 840-844. PMCID: PMC4538432
344. Holden, J. K.; Kang, S.; Beasley, F. C.; Cinelli, M. A.; Li, H.; Roy, S. G.; Dejam, D.; Edinger, A. L.; Nizet, V.; Silverman, R. B.; Poulos, T. L. Nitric oxide synthase as a target for methicillin resistant Staphylococcus aureus. Chem. Biol. 2015, 22, 785-892. PMCID: PMC4475277
345. Teixeira-Castro, A.; Jalles, A.; Esteves, S.; Kang, S.; da Silva Santos, L.; Silva-Fernandes, A.; Neto, M.; Brielmann, R. M.; Bessa, C.; Duarte-Silva, S.; Miranda, A.; Oliveira, S.; Neves-Carvalho, A.; Bessa, J.; Summavielle, T.; Silverman, R. B.; Oliveira, P.; Morimoto, R. I.; Maciel, P. Serotonergic signaling suppresses ataxin-3 aggregation and neurotoxicity in animal models of Machado-Joseph disease. Brain, 2015, 138, 3221-3237.
346. Xie, C. B.; Shaikh, L. H.; Garg, S.; Tanriver, G.; Teo, A. E. D.; Zhou, J.; Maniero, C.; Zhao, W.; Kang, S.; Silverman, R. B.; Azizan, E. A. B.; Brown, M. J. Regulation of aldosterone secretion by Cav1.3. Scientific Repts. 2016, srep24697. NIHR/UK funding
347. Holden, J. K.; Dejam, D.; Lewis, M. C.; Huang, H.; Kang, S.; Jing, Q.; Xue, F.; Silverman, R. B.; Poulos, T. L. Inhibitor bound crystal structures of bacterial nitric oxide synthase. Biochemistry, 2015, 54, 4075-4082.
348. Kang, S.; Li, H.; Tang, W.; Martásek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. 2-Aminopyridines with a truncated side chain to improve human neuronal nitric oxide synthase inhibitory potency and selectivity. J. Med. Chem. 2015, 58, 5548-5560. PMCID: PMC4514563
349. Zhang, Y.; Zhao, K. T.; Fox, S. G.; Kim, J.; Kirsch, D. R.; Ferrante, R. J.; Morimoto, R. I.; Silverman, R. B. Tertiary amine pyrazolones and their salts as inhibitors of mutant superoxide dismutase 1-dependent protein aggregation for the treatment of amyotrophic lateral sclerosis. J. Med. Chem. 2015, 58, 5942-5949. PMCID: PMC4537347
350. Cinelli, M. A.; Li, H.; Pensa, A. V.; Kang, S.; Roman, L. J.; Martasek, P.; Poulos, T. L.; Silverman, R. B. Phenyl ether- and aniline-containing 2-aminoquinolines as potent and selective inhibitors of neuronal nitric oxide synthase. J. Med. Chem. 2015, 58, 8694-8712.PMCID: PMC4644118
351. Silverman, R. B. Basic science to blockbuster drug: invention of pregabalin (Lyrica®). Technol. Innov. 2016, 17, 153-158.
352. Wang, H.-Y.; Qin, Y.; Li, H.; Roman, L. J.; Martásek, P.; Poulos, T. L. Potent and selective human neuronal nitric oxide synthase inhibition by optimization of the 2-aminopyridine-based scaffold with a pyridine linker. J. Med. Chem. 2016, 59, 4913-4925. PMCID: PMC4882237
353. Li, H.; Wang, H.-Y.; Kang, S.; Silverman, R. B.; Poulos, T. L. Electrostatic control of isoform selective inhibitor binding in nitric oxide synthase. Biochemistry 2016, 55, 3702-3707.
354. Holden, J. K.; Lewis, M. C.; Cinelli, M. A.; Abdullatif, Z.; Pensa, A. V.; Silverman, R. B.; Poulos, T. L. Targeting Bacterial Nitric Oxide Synthase with Aminoquinoline-based Inhibitors. Biochemistry 2016, 55, 5587-5594.
355. Zheng, J.; Chen, L.; Schwake, M.; Silverman, R. B.; Krainc, D. Design and synthesis of potent qunazolines as selective b-glucocerebrosidase modulators. J. Med. Chem. 2016, 59, 8508-8520. PMCID: PMC5033727
356. Wu, R.; Sanishvili, R.; Belitsky, B. R.; Juncosa, J. I.; Le, H. V.; Lehrer, H. J. S.; Farley, M.; Silverman, R. B.; Petsko, G. A.; Ringe, D.; Liu, D. PLP and GABA trigger GabR-mediated transcription regulation in Bacillus subtilis via external aldimine formation. Proc. Natl. Acad. Sci. USA, 2017, 114, 3891-3896. PMCID: PMC5393194
357. Cinelli, M. A.; Li, H.; Chreifi, G.; Poulos, T. L.; Silverman, R. B. Nitrile In The Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors. J. Med. Chem., 2017, 60(9), 3958-3978. PMICD: PMC5567828
358. Pensa, A.; Cinelli, M. A.; Li, H.; Chreifi, G.; Mukherjee, P.; Roman, L. J.; Martásek, P.; Poulos, T. L.; Silverman, R. B. Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors. J. Med. Chem. 2017, 60, 7146-7165. PMCID: PMC5570656
359. Mascarenhas, R.; Le, H. V.; Clevenger, K. D.; Lehrer, H. J., Ringe, D.; Kelleher, N. L.; Silverman, R. B.; Liu, D. Selective targeting by a mechanism-based inactivator against PLP-dependent enzymes: mechanisms of inactivation and alternative turnover. Biochemistry 2017,56, 4951-4961. PMCID: PMC 5624218
360. Do, H. T.; Wang, H.-Y.; Li, H.; Chreifi, G.; Poulos, T. L.; Silverman, R. B. Improvement of cell permeability of human neuronal nitric oxide synthase inhibitors using potent and selective 2-aminopyridine-based scaffolds with a fluorobenzene linker. J. Med. Chem. 2017, 60, 9360-9375.
361. Juncosa, J. I.; Takaya, K.; Le, H. V.; Moschitto, M. J.; Weerawarna, P. M.; Mascarenhas, R.; Liu, D.; Dewey, S. L.; Silverman, R. B. Design and mechanism of (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid, a highly potent GABA aminotransferase inactivator for the treatment of addiction. J. Am. Chem. Soc. 2018, 140, 2151-2164. PMCID: PMC5812813
362. Zheng, J.; Chen, L.; Skinner, O. S.; Remis, J.; Lansbury, P.; Skerlj, R.; Mrosek, M.; Heunisch, U.; Krapp, S.; Charrow, J.; Schwake, M.; Kelleher, N. L.; Silverman, R. B.; Krainc, D. b-Glucocerebrosidase modulators promote dimerization of b-glucocerebrosidase and reveal an allosteric binding site. J. Am. Chem. Soc. 2018, 140, 5914-5924. PMCID: PMC6098685
363. Silverman, R. B. Design and mechanism of GABA aminotransferase inactivators, treatments for epilepsies and addictions. (invited) Chem. Rev. 2018, 118, 4037-4070. PMCID: PMC6098685
364. Miley, G. P.; Rote, J. C.; Silverman, R. B.; Kelleher, N. L.; Thomson, R. J. Total synthesis of tambromycin enabled by indole C-H functionalization. Org. Lett. 2018, 20, 2369-2373. PMCID: PMC5953429
365. Moschitto, M. J.; Silverman, R. B. Synthesis of (S)-3-amino-4-(difluoromethylenyl)-cyclopent-1-ene-1-carboxylic acid (OV329), a potent inactivator of γ-aminobutyric acid aminotransferase. Org. Lett. 2018, 20, 4589-4592. PMCID: PMC6262895
366. Li, H.; Evenson, R. J.; Chreifi, G.; Silverman, R. B.; Poulos, T. P. The Structural Basis for Isoform Selective Nitric Oxide Synthase Inhibition by Thiophene-2-Carboximidamides. Biochemistry, 2018, 57, 6319-6325. PMCID: PMC6282162
367. Zheng, J.; Jeon, S.; Jiang, W.; Burbulla, L.; Oevel, K.; Krainc, D.; Silverman, R. B. Conversion of Quinazoline Modulators from Inhibitors to Activators of β-Glucocerebrosidase. J. Med. Chem. 2019, 62, 1218-1230. PMCID: PMC6467782
367a. Zheng, J.; Jeon, S.; Jiang, W.; Burbulla, L.; Oevel, K.; Krainc, D.; Silverman, R. B. Correction to Conversion of Quinazoline Modulators from Inhibitors to Activators of β-Glucocerebrosidase. J. Med. Chem. 2019, 62, 2850.
368. Burbulla, L. F.; Jeon, S.; Zheng, J.; Song, P.; Silverman, R. B.; Krainc, D. A modulator of wild- type glucocerebrosidase improves pathogenic phenotypes in dopaminergic neuronal models of Parkinson’s disease. Science Transl. Med., 2019, 11(514), eaau6870. PMCID: PMC7359409
369. Do, H.T.; Li, H.; Chreifi, G.; Poulos, T. L.; Silverman, R. B. Optimization of blood brain barrier permeability with potent and selective human neuronal nitric oxide synthase inhibitors having a 2-aminopyridine scaffold. J. Med. Chem. 2019, 62, 2690-2707. PMCID: PMC6586428
370. Moschitto, M. J.; Doubleday, P. F.; Catlin, D. S.; Kelleher, N. L.; Liu, D.; Silverman, R. B. Mechanism of inactivation of ornithine aminotransferase by (1S,3S)-3-amino-4-(hexafluoropropan-2-ylidenyl)cyclopentane-1-carboxylic acid. J. Am. Chem. Soc. 2019, 141, 10711-10721. PMCID: PMC6754100
371. Cinelli, M. A.; Do, H. T.; Miley, G. P.; Silverman, R. B. Inducible nitric oxide synthase: regulation, structure, and inhibition. Med. Res. Rev. 2020, 40, 158-189. PMCID: PMC6908786
- Rey, S.; Maton, G.; Satake, S.; Llano, I.; Kang, S.; Surmeier, D. J.; Silverman, R. B.; Collin, T. Physiological involvement of presynaptic L-type voltage dependent calcium channels in GABA release of cerebellar molecular layer interneurons. J. Neurochem. 2020, 155 (4), 390-402. Funded by CNRS and Université de Paris.
- Cinelli, M. A.; Reidl, C. T.; Li, H.; Chreifi, G.; Poulos, T. L.; Silverman, R. B. First contact: 7-Phenyl-2-aminoquinolines, potent and selective neuronal nitric oxide synthase inhibitors that target an isoform-specific aspartate. J. Med. Chem. 2020, 63 (9), 4528–4554. PMCID: PMC7429991
- Catlin, D. S.; Reidl, C. T.; Trzupek, T. R.; Silverman, R. B.; Cannon, B.; Becker, D. P.; Liu, D. (S)-4-Amino-5-phenoxypentanoate designed as a potential selective agonist of the bacterial transcription factor GabR. Protein Sci. 2020, 29, 1816-1828. 10.1002/pro.3905.
- Shen, S.; Doubleday, P. F.; Weerawarna, P. M.; Zhu, W.; Kelleher, N. L.; Silverman, R. B. Mechanism-based design of 3-amino-4-halocyclopentenecarboxylic acids as inactivators of g-aminobutyric acid aminotransferase. ACS Med. Chem. Lett. 2020, 11, 1949-1955. PMCID: PMC7549257
- Zhu, W.; Doubleday, P. F.; Catlin, D. S.; Weerawarna, P. M.; Butrin, A.; Shen, S.; Wawrzak, Z.; Kelleher, N. L.; Liu, D.; Silverman, R. B. A remarkable difference that one fluorine atom confers on the mechanisms of inactivation of human ornithine aminotransferase by two cyclohexene analogues of g-aminobutyric acid. J. Am. Chem. Soc. 2020, 142, 4892-4903. PMCID: PMC713438
- Silverman, R. B. Drug discovery: ingenuity and serendipity…or is it the other way around? Med. Chem. Rev. 2020, 55, Chapter 1, pp. 1-28. http://dx.doi.org/10.29200/acsmedchemrev-v55.ch1
- Cooper, G.; Kang, S.; Perez-Rosello, T.; Guzman, J. N.; Galtieri, D.; Xie, Z.; Kondapalli, J.; Mordell, J.; Silverman, R. B.; Surmeier, D. J. A single amino acid determines the selectivity and efficacy of selective negative allosteric modulators of CaV1.3 L-type calcium channels.ACS Chem. Biol. 2020, 15, 2539-2550. PMCID: PMC7502546
- Butrin, A.; Beaupre, B.; Kadamandla, N.; Zhao, P.; Shen, S.; Silverman, R. B.; Moran, G. R.; Liu, D. Structural and kinetic analyses reveal the dual inhibition modes of human ornithine aminotransferase by (1S,S)-3-amino-4-(hexafluoropropan-2-ylidenyl)-cyclopentane-1-carboxylic acid (BisCF3).
ACS Chem. Biol. 2021,16, 67-75. PMCID: PMC8474141
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Genç, B.; Gautam, M.; Gözütok, Ö.; Dervishi, I.; Sanchez, S.; Goshu, G. M.; Koçak, N.; Xie, E.; Silverman, R. B.; Özdinler, P. H. Improving mitochondria and ER stability helps eliminate upper motor neuron degeneration that occurs due to mSOD1 toxicity and TDP-43 pathology. Clin. Transl. Med., 2021, 11, e336. PMCID: PMC789803
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Weerawarna, P. M.; Moschitto, M. J.; Silverman, R. B. Theoretical and mechanistic studies of the inactivation of GABA aminotransferase by OV329 and CPP-115. Determination of the rate-limiting step and validation of the global kinetic parameters. ACS Chem. Biol., 2021, 16, 615-630. PMCID: PMC837171
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Sadleir, K. R.; Popovoic, J.; Zhu, W.; Reidel, C. T.; Do, H.; Silverman, R. B.; Vassar, R. Pregabalin treatment does not affect amyloid pathology in 5XFAD mice. Curr. Alzheimer Res. 2021, 18, 283-297.https://doi.org/10.2174/1567205018666210713125333
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Shen, S.; Butrin, A.; Doubleday, P. F.; Melani, R. D.; Beaupre, B. A.; Tavares, M. T.; Ferreira, G. M.; Kelleher, N. L.; Moran, G. R.; Liu, D.; Silverman, R. B. Turnover and inactivation mechanisms for (S)-3-amino-4,4-difluorocyclopent-1-enecarboxylic acid, a selective mechanism-based inactivator of human ornithine aminotransferase. J. Am. Chem. Soc. 2021, 143, 8689-8703. PMCID: PMC836702
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Zhu, W.; Doubleday, P. F.; Butrin, A.; Weerawarna, P. M.; Melani, R.; Catlin, D. S.; Dwight, T. A.; Liu, D.; Kelleher, N. L.; Silverman, R. B. Remarkable and unexpected mechanism for (S)-3-amino-4-(difluoromethylenyl)cyclohex-1-ene-carboxylic acid as a selective inactivator of human ornithine aminotransferase. J. Am. Chem. Soc. 2021, 143, 8193-8207. PMCID: PMC836938
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Feja, M.; Meller, S.; Deking, L. S.; Kaczmarek, E.; During, M. J.; Silverman, R. B.; Gernert, M. OV329, a novel highly potent GABA aminotransferase inactivator, induces pronounced anticonvulsant effects in the pentylenetetrazole seizure threshold test and in amygdala-kindled rats. Epilepsia 2021, 00, 1-14.
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Silverman, R. B. Inactivators of ornithine aminotransferase for the treatment of hepatocellular carcinoma. ACS Med. Chem. Lett. 2022, 13, 38-49. PMCID: PMC8762738
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Tong, S.; Cinelli, M.; Ibrahim, N.; Huang, H.; Silverman, R. B.; Yang, S. Inhibition of interferon-gamma-stimulated melanoma progression by targeting neuronal nitric oxide synthase (nNOS). Scientific Reports, 2022, 12, 1701. PMCID: PMC8807785
- Genç, B.; Gautam, M.; Helmold, B.; Koçak, N.; Günay, A.; Goshu, G. M.; Silverman, R. B.; Özdinler P. H. NU-9 improves health of hSOD1G93A mouse upper motor neurons in vitro, especially in combination with riluzole or edaravone. Sci. Rep. 2022, 12, 5383. PMCID: PMC8967818
- Yun, J.; Jeong, D.; Xie, Z.; Lee, S.; Surmeier, D. J.; Silverman, R. B.; Kang, S. Palladium-catalyzed a-arylation of cyclic b-dicarbonyl compounds for the synthesis of CaV1.3 inhibitors. ACS Omega, 2022, 7, 14252-14263. PMCID: PMC9089348
- Tong, S; Darwish, S.; Ariani, H. H.; Lozada, K. A.; Salehi, D.; Silverman, R. B.; Kaur, K.; Yang, S. A small peptide increases drug delivery in human melanoma cells. Pharmaceutics, 2022, 14, 1026. PMCID: PMC9145755
- Zhu, W.; Butrin, A.; Melani, R. D.; Doubleday, P. F.; Ferreira, G. M.; Tavares, M. T.; Habeeb Mohammad, T. S.; Beaupre, B. A.; Kelleher, N. L.; Moran, G. R.; Liu, D.; Silverman, R. B. Rational design, synthesis, and mechanism of (3S,4R)-3-amino-4-(difluoromethyl)cyclopent-1-ene-1-carboxylic acid: employing a second deprotonation strategy for selectivity of hOAT over GABA-AT. J. Am. Chem. Soc., 2022, 144, 5629-5642. PMCID: PMC9181902.391a. Correction to Zhu, W.; Butrin, A.; Melani, R. D.; Doubleday, P. F.; Ferreira, G. M.; Tavares, M. T.; Habeeb Mohammad, T. S.; Beaupre, B. A.; Kelleher, N. L.; Moran, G. R.; Liu, D.; Silverman, R. B. Rational design, synthesis, and mechanism of (3S,4R)-3-amino-4-(difluoromethyl)cyclopent-1-ene-1-carboxylic acid: employing a second deprotonation strategy for selectivity of hOAT over GABA-AT. J. Am. Chem. Soc. 2023, 145, 9895-9896.
- Vasu, D.; Li, H.; Hardy, C. D.; Poulos, T. L.; Silverman, R. B. 2-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors. Bioorg. Med. Chem. 2022, 69, 116878. PMCID: PMC9574886
- Shen, S.; Butrin, A.; Beaupre, B. A.; Ferreira, G. M.; Doubleday, P. F.; Grass, D. H.; Zhu, W.; Kelleher, N. L.; Moran, G. R.; Liu, D.; Silverman, R. B. Structural and mechanistic basis for the inactivation of human ornithine aminotransferase by (3S,4S)-3-amino-4-fluorocyclopentenecarboxylic acid. Molecules 2023, 28(3), 1133. PMCID: PMC9921285
- Elmansy, M. F.; Reidl, C. T.; Rahaman, M.; Özdinler, P. H.; Silverman, R. B. Small molecules targeting different cellular pathologies for the treatment of amyotrophic lateral sclerosis. Med. Res. Rev. 2023, 43(6), 260-2302. https://doi.org/10.1002/med.21974. PMCID: PMC10592673
- Lykins, J.; Moschitto, M. J.; Zhou, Y.; Filippova, E. V.; Le, H. V.; Tomita, T.; Fox, B. A.; Bzik, D.; Su, C.; Rajagopala, S. V.; Flores, K.; Spano, F.; Woods, S.; Roberts, C. W.; Hua, C.; El Bissati, K.; Wheeler, K. M.; Dovgin, S.; Muench, S. P.; McPhillie, M.; Fishwick, C. W. G.; Anderson, W. F.; Lee, P.; Hickman, M.; Weiss, L. M.; Dubey, J. P.; Lorenzi, H.; Silverman, R. B.; McLeod, R. L. From TgO/GABA-AT, GABA and T-263 mutant to conception of Toxoplasma, iScience 2023, 27(1), 108477. doi: https://doi.org/10.1016/j.isci.2023.108477. PMCID: PMC10776954
- Weerawarna, P. M.; Schiefer, I. T.; Fox, S.; Morimoto, R. I.; Melani, R. D.; Kelleher, N. L.; Luan, C.-H.; Silverman, R. B. Target identification of a class of pyrazolone protein aggregation inhibitor therapeutics for amyotrophic lateral sclerosis. ACS Central Sci. 2023, 10(1), 87-103. DOI: 10.1021/acscentsci.3c00213. PMCID: PMC10823514
- Vasu, D.; Reidl, C. T.; Wang, E.; Yang, S.; Silverman, R. B. Improved synthesis and anticancer activity of a potent neuronal nitric oxide synthase inhibitor. Bioorg. Med. Chem. Lett. 2023, 90, 129329. https://doi.org/10.1016/j.bmcl.2023.129329. PMCID: PMC10330524
- Vasu, D.; Do, H. T.; Li, H.; Hardy, C. D.; Poulos, T. L.; Silverman, R. B. Potent, selective, and membrane permeable 2-amino-4-substituted pyridine-based neuronal nitric oxide synthase inhibitors. J. Med. Chem. 2023, 66, 9934-9953. doi: 10.1021/acs.jmedchem.3c00782. PMCID: PMC10824152
- Li, H.; Hardy, C. D.; Reidl, C. T.; Jing, Q.; Xue, F.; Cinelli, M.; Silverman, R. B.; Poulos, T. L. Crystallographic and computational insights into isoform-selective dynamics in nitric oxide synthase. Biochemistry 2024, 63(6), 788-796. PMCID: PMC10956423
- Devitt, A. N.; Vargas, A. L.; Zhu, W.; Des Soye, B. J.; Butun, F. A.; Alt, T.; Kaley, N.; Ferreira, G. M.; Moran, G.; Kelleher, N. L.; Liu, D.; Silverman, R. B. Design, Synthesis, and Mechanistic Studies of (R)-3-Amino-5,5-difluorocyclohex-1-ene-1-carboxylic Acid as an Inactivator of Human Ornithine Aminotransferase. ACS Chem. Biol. 2024, 19(5), 1066-1081. PMCID: PMC11274680
- Dukes, A. O.; Weerawarna, P. M.; Devitt, A. N.; Silverman, R. B. Synthesis of (2R,4S)-4-amino-5-hydroxybicyclo[3.1.1]heptane-2-carboxylic acid via an asymmetric intramolecular Mannich reaction. J. Org. Chem. 2024, 89, 9110-9117. PMCID: PMC11418922
- Wirt, J. L.; Assis Ferreira, L.; Jesus, C. H. A.; Woodward, T. J.; Oliva, I.; Xu, Z.; Crystal, J. D.; Pepin, R. H.; Silverman, R. B.; Hohmann, A. G. Efficacy of GABA aminotransferase inactivator OV329 in models of neuropathic and inflammatory pain without tolerance or addiction. Proc. Natl. Acad. Sci. USA 2025, 122(1), e2318833121; https://doi.org/10.1073/pnas.2318833121. PMCID: PMC11725897