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Research Output 1968 2020

2020
8 Citations (Scopus)

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

Nitric Oxide Synthase Type II
Sepsis
Nitric Oxide
Protein Isoforms
Inhibition (Psychology)
2019
2 Citations (Scopus)
Glucosylceramidase
Parkinson Disease
Phenotype
Mutation
Synucleins
3 Citations (Scopus)

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

Zheng, J., Jeon, S., Jiang, W., Burbulla, L., 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

Glucosylceramidase
Quinazolines
Parkinson Disease
Mutant Proteins
Structure-Activity Relationship
Aminoquinolines
Nitric Oxide Synthase Type I
Nitriles
Pharmaceutical Chemistry
Bistris
Fluorobenzenes
Nitric Oxide Synthase Type I
Pharmaceutical Chemistry
Permeability
alpha-aminopyridine
Glucosylceramidase
Quinazolines

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

Ornithine-Oxo-Acid Transaminase
Cyclopentanes
Carboxylic Acids
Transaminases
Fluorides

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

Nitric Oxide Synthase Type I
Blood-Brain Barrier
Permeability
Central Nervous System Agents
P-Glycoprotein
2018
9 Citations (Scopus)

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

4-Aminobutyrate Transaminase
Aminobutyrates
Carboxylic Acids
Transaminases
Carboxylic acids
5 Citations (Scopus)

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

4-Aminobutyrate Transaminase
gamma-Aminobutyric Acid
Aminobutyrates
Enzymes
Neurotransmitter Agents
1 Citation (Scopus)

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

Thiophenes
Nitric Oxide Synthase Type I
Nitric Oxide Synthase
Protein Isoforms
Aminopyridines
2 Citations (Scopus)
Aminobutyrates
Cyclopentanes
Poisons
Selenium
Carboxylic Acids
10 Citations (Scopus)

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

indoles
Amination
synthesis
Biological Products
fragments
7 Citations (Scopus)

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

Glucosylceramidase
Allosteric Site
Dimerization
Binding sites
Modulators
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

6 Citations (Scopus)

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

Aminoquinolines
Nitric Oxide Synthase Type I
Methylation
Biological Availability
Arginine
5 Citations (Scopus)

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

Fluorobenzenes
Nitric Oxide Synthase Type I
Permeability
Protein Isoforms
Cell Membrane Permeability
10 Citations (Scopus)

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

Aminoquinolines
Nitric Oxide Synthase Type I
Nitriles
Permeability
Membranes
10 Citations (Scopus)

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

Pyridoxal Phosphate
Bacillus subtilis
gamma-Aminobutyric Acid
Transcriptional Activation
4-Aminobutyrate Transaminase
2 Citations (Scopus)

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

Pyridoxal Phosphate
Ornithine-Oxo-Acid Transaminase
Aspartate Aminotransferases
Enzymes
Crystal structure
2016
5 Citations (Scopus)

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

Glucosylceramidase
Quinazolines
Gaucher Disease
Parkinson Disease
Lewy Body Disease
1 Citation (Scopus)

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

Static Electricity
Nitric Oxide Synthase
Electrostatics
Protein Isoforms
Aminopyridines
1 Citation (Scopus)

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

Aminoquinolines
Nitric Oxide Synthase Type I
phenyl ether
aniline
11 Citations (Scopus)

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

Nitric Oxide Synthase Type I
Liver Microsomes
Protein Binding
Neurodegenerative Diseases
Cytochrome P-450 Enzyme System
18 Citations (Scopus)

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

Aldosterone
Adenoma
Zona Glomerulosa
L-Type Calcium Channels
Nifedipine
9 Citations (Scopus)

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

Aminoquinolines
Nitric Oxide Synthase
Scaffolds
Bacillus anthracis
Mutagenesis
2015
12 Citations (Scopus)

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

Nitric Oxide Synthase Type I
Diamines
Biological Availability
alpha-aminopyridine
Catalytic Domain
Aminopyridines
Nitric Oxide Synthase Type I
Dimers
Chemical analysis
7 Citations (Scopus)

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

Sirtuin 2
Derivatives
Sulfonamides
Sulfides
sulfoxide
9 Citations (Scopus)

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

Aminobutyrates
Transaminases
gamma-Aminobutyric Acid
Acids
Brain
4 Citations (Scopus)

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

Bacterial Structures
Nitric Oxide Synthase
Crystal structure
Oxidative stress
Catalytic Domain

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

5 Citations (Scopus)

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

4-Aminobutyrate Transaminase
Acids
gamma-Aminobutyric Acid
Vigabatrin
Metabolites
2 Citations (Scopus)

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

Nitric Oxide Synthase Type I
Nitric oxide
Heme
Nitric Oxide Synthase
Acids
10 Citations (Scopus)

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

Aminobutyrates
Transaminases
gamma-Aminobutyric Acid
Phosphates
Coulomb interactions
6 Citations (Scopus)

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

Amidines
Nitric Oxide Synthase Type II
Heme
Biliverdine
Substrates
11 Citations (Scopus)

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

Methicillin
Methicillin-Resistant Staphylococcus aureus
Nitric Oxide Synthase
Crystal structure
Mutagenesis
15 Citations (Scopus)

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

Pyrimidines
Nitric Oxide Synthase Type I
Biological Availability
Liver Microsomes
Cytochromes
13 Citations (Scopus)

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

Ornithine-Oxo-Acid Transaminase
4-Aminobutyrate Transaminase
Pharmaceutical Preparations
gamma-Aminobutyric Acid
Aminobutyrates
13 Citations (Scopus)

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

Aminoquinolines
Nitric Oxide Synthase Type I
Permeability
Nitric Oxide
Neurodegenerative Diseases
30 Citations (Scopus)

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

Machado-Joseph Disease
Citalopram
Animal Models
Caenorhabditis elegans
Serotonin Plasma Membrane Transport Proteins
10 Citations (Scopus)

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

Nitric Oxide Synthase
Pterins
Catalytic Domain
Protein Isoforms
Bacillus anthracis
14 Citations (Scopus)

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

Ornithine-Oxo-Acid Transaminase
Hepatocellular Carcinoma
4-Aminobutyrate Transaminase
alpha-Fetoproteins
Genes
8 Citations (Scopus)

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

Mevalonic Acid
Plasma stability
Prodrugs
pyrophosphomevalonate decarboxylase
Amidohydrolases
5 Citations (Scopus)

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

Pyrazolones
Amyotrophic Lateral Sclerosis
Amines
Salts
Structure-Activity Relationship
3 Citations (Scopus)

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

Pharmaceutical Preparations
Organic Chemicals
Organic Chemistry
Molecules
Pharmaceutical Chemistry
57 Citations (Scopus)

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

Sirtuin 2
Parkinson disease
Amyotrophic Lateral Sclerosis
ischemia
Brain Ischemia
2014
10 Citations (Scopus)

Accessible chiral linker to enhance potency and selectivity of neuronal nitric oxide synthase inhibitors

Jing, Q., Li, H., Roman, L. J., Martásek, P., Poulos, T. L. & Silverman, R. B., Jan 9 2014, In : ACS Medicinal Chemistry Letters. 5, 1, p. 56-60 5 p.

Research output: Contribution to journalArticle

Nitric Oxide Synthase Type I
Propionates
Heme
Isoenzymes
Hydrogen
9 Citations (Scopus)

Combination of chiral linkers with thiophenecarboximidamide heads to improve the selectivity of inhibitors of neuronal nitric oxide synthase

Jing, Q., Li, H., Roman, L. J., Martásek, P., Poulos, T. L. & Silverman, R. B., Sep 15 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 18, p. 4504-4510 7 p.

Research output: Contribution to journalArticle

Nitric Oxide Synthase Type I
Propionates
Drug Discovery
Heme
Biological Availability