• 10272 Citations
1968 …2024

Research output per year

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Research Output

2020

A Remarkable Difference That One Fluorine Atom Confers on the Mechanisms of Inactivation of Human Ornithine Aminotransferase by Two Cyclohexene Analogues of γ-Aminobutyric Acid

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., Mar 11 2020, In : Journal of the American Chemical Society. 142, 10, p. 4892-4903 12 p.

Research output: Contribution to journalArticle

First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate

Cinelli, M. A., Reidl, C. T., Li, H., Chreifi, G., Poulos, T. L. & Silverman, R. B., Jan 1 2020, (Accepted/In press) In : Journal of Medicinal Chemistry.

Research output: Contribution to journalArticle

Inducible nitric oxide synthase: Regulation, structure, and inhibition

Cinelli, M. A., Do, H. T., Miley, G. P. & Silverman, R. B., Jan 1 2020, In : Medicinal Research Reviews. 40, 1, p. 158-189 32 p.

Research output: Contribution to journalReview article

12 Scopus citations

Mechanism-Based Design of 3-Amino-4-Halocyclopentenecarboxylic Acids as Inactivators of GABA Aminotransferase

Shen, S., Doubleday, P. F., Weerawarna, P. M., Zhu, W., Kelleher, N. L. & Silverman, R. B., Jan 1 2020, (Accepted/In press) In : ACS Medicinal Chemistry Letters.

Research output: Contribution to journalArticle

2019
4 Scopus citations

Conversion of Quinazoline Modulators from Inhibitors to Activators of β-Glucocerebrosidase

Zheng, J., Jeon, S., Jiang, W., Burbulla, L. F., Ysselstein, D., Oevel, K., Krainc, D. & Silverman, R. B., Feb 14 2019, In : Journal of Medicinal Chemistry. 62, 3, p. 1218-1230 13 p.

Research output: Contribution to journalArticle

4 Scopus citations

Mechanism of Inactivation of Ornithine Aminotransferase by (1 S,3 S)-3-Amino-4-(hexafluoropropan-2-ylidenyl)cyclopentane-1-carboxylic Acid

Moschitto, M. J., Doubleday, P. F., Catlin, D. S., Kelleher, N. L., Liu, D. & Silverman, R. B., Jul 10 2019, In : Journal of the American Chemical Society. 141, 27, p. 10711-10721 11 p.

Research output: Contribution to journalArticle

1 Scopus citations

Optimization of Blood-Brain Barrier Permeability with Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibitors Having a 2-Aminopyridine Scaffold

Do, H. T., Li, H., Chreifi, G., Poulos, T. L. & Silverman, R. B., Mar 14 2019, In : Journal of Medicinal Chemistry. 62, 5, p. 2690-2707 18 p.

Research output: Contribution to journalArticle

3 Scopus citations
2018

Design and Mechanism of (S)-3-Amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic Acid, a Highly Potent γ-Aminobutyric Acid Aminotransferase Inactivator for the Treatment of Addiction

Juncosa, J. I., Takaya, K., Le, H. V., Moschitto, M. J., Weerawarna, P. M., Mascarenhas, R., Liu, D., Dewey, S. L. & Silverman, R. B., Feb 14 2018, In : Journal of the American Chemical Society. 140, 6, p. 2151-2164 14 p.

Research output: Contribution to journalArticle

11 Scopus citations

Design and mechanism of GABA aminotransferase inactivators. Treatments for epilepsies and addictions

Silverman, R. B., Apr 11 2018, In : Chemical Reviews. 118, 7, p. 4037-4070 34 p.

Research output: Contribution to journalReview article

8 Scopus citations

Structural Basis for Isoform Selective Nitric Oxide Synthase Inhibition by Thiophene-2-carboximidamides

Li, H., Evenson, R. J., Chreifi, G., Silverman, R. B. & Poulos, T. L., Nov 6 2018, In : Biochemistry. 57, 44, p. 6319-6325 7 p.

Research output: Contribution to journalArticle

2 Scopus citations
3 Scopus citations

Total Synthesis of Tambromycin Enabled by Indole C-H Functionalization

Miley, G. P., Rote, J. C., Silverman, R. B., Kelleher, N. L. & Thomson, R. J., Apr 20 2018, In : Organic Letters. 20, 8, p. 2369-2373 5 p.

Research output: Contribution to journalArticle

11 Scopus citations

β-Glucocerebrosidase Modulators Promote Dimerization of β-Glucocerebrosidase and Reveal an Allosteric Binding Site

Zheng, J., Chen, L., Skinner, O. S., Ysselstein, D., Remis, J., Lansbury, P., Skerlj, R., Mrosek, M., Heunisch, U., Krapp, S., Charrow, J., Schwake, M., Kelleher, N. L., Silverman, R. B. & Krainc, D., May 9 2018, In : Journal of the American Chemical Society. 140, 18, p. 5914-5924 11 p.

Research output: Contribution to journalArticle

8 Scopus citations
2017

Basic science to blockbuster drug: invention of pregabalin (Lyrica®)

Silverman, R. B., 2017, In : Technology and Innovation. 17, p. 153-158 6 p.

Research output: Contribution to journalArticle

Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors

Pensa, A. V., Cinelli, M. A., Li, H., Chreifi, G., Mukherjee, P., Roman, L. J., Martásek, P., Poulos, T. L. & Silverman, R. B., Aug 24 2017, In : Journal of Medicinal Chemistry. 60, 16, p. 7146-7165 20 p.

Research output: Contribution to journalArticle

8 Scopus citations

Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker

Do, H. T., Wang, H. Y., Li, H., Chreifi, G., Poulos, T. L. & Silverman, R. B., Nov 22 2017, In : Journal of Medicinal Chemistry. 60, 22, p. 9360-9375 16 p.

Research output: Contribution to journalArticle

7 Scopus citations

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

Cinelli, M. A., Li, H., Chreifi, G., Poulos, T. L. & Silverman, R. B., May 11 2017, In : Journal of Medicinal Chemistry. 60, 9, p. 3958-3978 21 p.

Research output: Contribution to journalArticle

13 Scopus citations

PLP and GABA trigger GabR-mediated transcription regulation in Bacillus subtilis via external aldimine formation

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., Apr 11 2017, In : Proceedings of the National Academy of Sciences of the United States of America. 114, 15, p. 3891-3896 6 p.

Research output: Contribution to journalArticle

11 Scopus citations

Selective Targeting by a Mechanism-Based Inactivator against Pyridoxal 5′-Phosphate-Dependent Enzymes: Mechanisms of Inactivation and Alternative Turnover

Mascarenhas, R., Le, H. V., Clevenger, K. D., Lehrer, H. J., Ringe, D., Kelleher, N. L., Silverman, R. B. & Liu, D., Sep 19 2017, In : Biochemistry. 56, 37, p. 4951-4961 11 p.

Research output: Contribution to journalArticle

4 Scopus citations
2016

Design and Synthesis of Potent Quinazolines as Selective β-Glucocerebrosidase Modulators

Zheng, J., Chen, L., Schwake, M., Silverman, R. B. & Krainc, D., Sep 22 2016, In : Journal of Medicinal Chemistry. 59, 18, p. 8508-8520 13 p.

Research output: Contribution to journalArticle

5 Scopus citations

Electrostatic Control of Isoform Selective Inhibitor Binding in Nitric Oxide Synthase

Li, H., Wang, H. Y., Kang, S., Silverman, R. B. & Poulos, T. L., Jul 5 2016, In : Biochemistry. 55, 26, p. 3702-3707 6 p.

Research output: Contribution to journalArticle

2 Scopus citations

Erratum: Phenyl Ether- and Aniline-Containing 2-Aminoquinolines as Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase (J. Med. Chem. (2015) 58:21 (8694?8712) DOI: 10.1021/acs.jmedchem.5b01330)

Cinelli, M. A., Li, H., Pensa, A. V., Kang, S., Roman, L. J., Martásek, P., Poulos, T. L. & Silverman, R. B., Feb 11 2016, In : Journal of Medicinal Chemistry. 59, 3, 1 p.

Research output: Contribution to journalComment/debate

1 Scopus citations

Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibition by Optimization of the 2-Aminopyridine-Based Scaffold with a Pyridine Linker

Wang, H. Y., Qin, Y., Li, H., Roman, L. J., Martásek, P., Poulos, T. L. & Silverman, R. B., May 26 2016, In : Journal of Medicinal Chemistry. 59, 10, p. 4913-4925 13 p.

Research output: Contribution to journalArticle

11 Scopus citations

Regulation of aldosterone secretion by Ca v 1.3

Xie, C. B., Haris Shaikh, L., 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., Apr 21 2016, In : Scientific reports. 6, 24697.

Research output: Contribution to journalArticle

20 Scopus citations

Targeting Bacterial Nitric Oxide Synthase with Aminoquinoline-Based Inhibitors

Holden, J. K., Lewis, M. C., Cinelli, M. A., Abdullatif, Z., Pensa, A. V., Silverman, R. B. & Poulos, T. L., Oct 4 2016, In : Biochemistry. 55, 39, p. 5587-5594 8 p.

Research output: Contribution to journalArticle

10 Scopus citations
2015

2-Aminopyridines with a Truncated Side Chain to Improve Human Neuronal Nitric Oxide Synthase Inhibitory Potency and Selectivity

Kang, S., Li, H., Tang, W., Martásek, P., Roman, L. J., Poulos, T. L. & Silverman, R. B., Jul 23 2015, In : Journal of Medicinal Chemistry. 58, 14, p. 5548-5560 13 p.

Research output: Contribution to journalArticle

12 Scopus citations

Design and evaluation of 3-(benzylthio)benzamide derivatives as potent and selective SIRT2 inhibitors

Khanfar, M. A., Quinti, L., Wang, H., Nobles, J., Kazantsev, A. G. & Silverman, R. B., May 14 2015, In : ACS Medicinal Chemistry Letters. 6, 5, p. 607-611 5 p.

Research output: Contribution to journalArticle

7 Scopus citations

Design and Mechanism of Tetrahydrothiophene-Based γ-Aminobutyric Acid Aminotransferase Inactivators

Le, H. V., Hawker, D. D., Wu, R., Doud, E., Widom, J., Sanishvili, R., Liu, D., Kelleher, N. L. & Silverman, R. B., Mar 17 2015, In : Journal of the American Chemical Society. 137, 13, p. 4525-4533 9 p.

Research output: Contribution to journalArticle

9 Scopus citations

Inhibitor Bound Crystal Structures of Bacterial Nitric Oxide Synthase

Holden, J. K., Dejam, D., Lewis, M. C., Huang, H., Kang, S., Jing, Q., Xue, F., Silverman, R. B. & Poulos, T. L., Jul 7 2015, In : Biochemistry. 54, 26, p. 4075-4082 8 p.

Research output: Contribution to journalArticle

4 Scopus citations

Manuale di chimica farmaceutica: Progettazione, meccanismo d'azione e metabolismo dei farmaci

Silverman, R. B., Holladay, M. W., Almerico, A. M. (Translator), Di Stilo, A. (Translator), Fruttero, R. (Translator), Lauria, A. (Translator), Murineddu, G. (Translator), Pinna, G. (Translator) & Pinnen, F. (Translator), 2015, 3 ed. Milano: Edra. 446 p.

Research output: Book/ReportBook

Mechanism of Inactivation of GABA Aminotransferase by (E)- and (Z)-(1S,3S)-3-Amino-4-fluoromethylenyl-1-cyclopentanoic Acid

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., Sep 18 2015, In : ACS chemical biology. 10, 9, p. 2087-2098 12 p.

Research output: Contribution to journalArticle

5 Scopus citations

Mechanism of Inactivation of Neuronal Nitric Oxide Synthase by (S)-2-Amino-5-(2-(methylthio)acetimidamido)pentanoic Acid

Tang, W., Li, H., Doud, E. H., Chen, Y., Choing, S., Plaza, C., Kelleher, N. L., Poulos, T. L. & Silverman, R. B., May 13 2015, In : Journal of the American Chemical Society. 137, 18, p. 5980-5989 10 p.

Research output: Contribution to journalArticle

2 Scopus citations

Mechanism of inactivation of γ-aminobutyric acid aminotransferase by (1 S,3 S)-3-amino-4-difluoromethylene-1-cyclopentanoic acid (CPP-115)

Lee, H., Doud, E. H., Wu, R., Sanishvili, R., Juncosa, J. I., Liu, D., Kelleher, N. L. & Silverman, R. B., Feb 25 2015, In : Journal of the American Chemical Society. 137, 7, p. 2628-2640 13 p.

Research output: Contribution to journalArticle

13 Scopus citations

Mechanistic studies of inactivation of inducible nitric oxide synthase by amidines

Tang, W., Li, H., Poulos, T. L. & Silverman, R. B., Apr 21 2015, In : Biochemistry. 54, 15, p. 2530-2538 9 p.

Research output: Contribution to journalArticle

7 Scopus citations

Nitric Oxide Synthase as a Target for Methicillin-Resistant Staphylococcus aureus

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., Jun 20 2015, In : Chemistry and Biology. 22, 6, p. 785-792 8 p.

Research output: Contribution to journalArticle

11 Scopus citations

Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase

Mukherjee, P., Li, H., Sevrioukova, I., Chreifi, G., Martásek, P., Roman, L. J., Poulos, T. L. & Silverman, R. B., Feb 12 2015, In : Journal of Medicinal Chemistry. 58, 3, p. 1067-1088 22 p.

Research output: Contribution to journalArticle

17 Scopus citations

Ornithine aminotransferase versus GABA aminotransferase: Implications for the design of new anticancer drugs

Lee, H., Juncosa, J. I. & Silverman, R. B., Mar 1 2015, In : Medicinal Research Reviews. 35, 2, p. 286-305 20 p.

Research output: Contribution to journalArticle

15 Scopus citations

Phenyl ether- and aniline-containing 2-aminoquinolines as potent and selective inhibitors of neuronal nitric oxide synthase

Cinelli, M. A., Li, H., Pensa, A. V., Kang, S., Roman, L. J., Martásek, P., Poulos, T. L. & Silverman, R. B., Nov 12 2015, In : Journal of Medicinal Chemistry. 58, 21, p. 8694-8712 19 p.

Research output: Contribution to journalArticle

15 Scopus citations

Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease

Teixeira-Castro, A., Jalles, A., Esteves, S., Kang, S., Da Silva Santos, L., Silva-Fernandes, A., Neto, M. F., 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., Nov 2015, In : Brain. 138, 11, p. 3221-3237 17 p.

Research output: Contribution to journalArticle

34 Scopus citations

Structure-based design of bacterial nitric oxide synthase inhibitors

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., Jan 22 2015, In : Journal of Medicinal Chemistry. 58, 2, p. 994-1004 11 p.

Research output: Contribution to journalArticle

11 Scopus citations

Suppression of Hepatocellular Carcinoma by Inhibition of Overexpressed Ornithine Aminotransferase

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., Aug 13 2015, In : ACS Medicinal Chemistry Letters. 6, 8, p. 840-844 5 p.

Research output: Contribution to journalArticle

15 Scopus citations

Synthesis of mevalonate-and fluorinated mevalonate prodrugs and their in vitro human plasma stability

Kang, S., Watanabe, M., Jacobs, J. C., Yamaguchi, M., Dahesh, S., Nizet, V., Leyh, T. S. & Silverman, R. B., Jan 27 2015, In : European Journal of Medicinal Chemistry. 90, p. 448-461 14 p.

Research output: Contribution to journalArticle

8 Scopus citations

Tertiary Amine Pyrazolones and Their Salts as Inhibitors of Mutant Superoxide Dismutase 1-Dependent Protein Aggregation for the Treatment of Amyotrophic Lateral Sclerosis

Zhang, Y., Zhao, K. T., Fox, S. G., Kim, J., Kirsch, D. R., Ferrante, R. J., Morimoto, R. I. & Silverman, R. B., Jul 17 2015, In : Journal of Medicinal Chemistry. 58, 15, p. 5942-5949 8 p.

Research output: Contribution to journalArticle

5 Scopus citations

The Organic Chemistry of Drug Design and Drug Action: Third Edition

Silverman, R. B. & Holladay, M. W., Jan 1 2015, Elsevier Inc. 517 p.

Research output: Book/ReportBook

4 Scopus citations

The sirtuin-2 inhibitor AK7 is neuroprotective in models of parkinson's disease but not amyotrophic lateral sclerosis and cerebral ischemia

Chen, X., Wales, P., Quinti, L., Zuo, F., Moniot, S., Herisson, F., Rauf, N. A., Wang, H., Silverman, R. B., Ayata, C., Maxwell, M. M., Steegborn, C., Schwarzschild, M. A., Outeiro, T. F. & Kazantsev, A. G., Jan 21 2015, In : PloS one. 10, 1, e0116919.

Research output: Contribution to journalArticle

59 Scopus citations