Keyword

isoform selectivity

Description: The degree to which a molecule, such as a drug or inhibitor, preferentially interacts with one protein isoform over others.

Primary topic: Enzyme function and inhibition (26%)

OpenAlex ID: keywords/isoform-selectivity

Chemical phylogenetics of histone deacetylases

2010 · James E Bradner, Nathan West, et al. · Nature Chemical Biology · 713

Evolution of NADPH Oxidase Inhibitors: Selectivity and Mechanisms for Target Engagement

2014 · Sebastian Altenhöfer, Kim A. Radermacher, et al. · Antioxidants and Redox Signaling · 519

PDF

Nitric oxide: A radical neurotransmitter in the central nervous system

1994 · Steven R. Vincent · Progress in Neurobiology · 463

Identification of PKC-isoform-specific biological actions using pharmacological approaches

2000 · Kerrie J Way, Eva Chou, et al. · Trends in Pharmacological Sciences · 436

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165

2019 · Stephen T. Wrobleski, Ryan Moslin, et al. · Journal of Medicinal Chemistry · 383

Inside HDAC with HDAC inhibitors

2010 · Philippe Bertrand · European Journal of Medicinal Chemistry · 352

Isoform-selective histone deacetylase inhibitors

2008 · Anton V. Bieliauskas, Mary Kay H. Pflum · Chemical Society Reviews · 346

Ex-527 inhibits Sirtuins by exploiting their unique NAD + -dependent deacetylation mechanism

2013 · Melanie Gertz, Frank Fischer, et al. · Proceedings of the National Academy of Sciences · 317

PDF

The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors

2010 · Alex Berndt, Simon Miller, et al. · Nature Chemical Biology · 292

Conformational Restriction: An Effective Tactic in ‘Follow-On’-Based Drug Discovery

2014 · Zengjun Fang, Yu’ning Song, et al. · Future Medicinal Chemistry · 268

Role of a Novel PH-Kinase Domain Interface in PKB/Akt Regulation: Structural Mechanism for Allosteric Inhibition

2009 · Véronique Calleja, Michel Laguerre, et al. · PLoS Biology · 251

PDF

NADPH oxidases in the vasculature: Molecular features, roles in disease and pharmacological inhibition

2008 · Stavros Selemidis, Christopher G. Sobey, et al. · Pharmacology & Therapeutics · 242

Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation

2017 · Chiara Maniaci, Scott J. Hughes, et al. · Nature Communications · 241

PDF

Inflammation and Hypoxia: HIF and PHD Isoform Selectivity

2018 · Emily R. Watts, Sarah R. Walmsley · Trends in Molecular Medicine · 237

PDF

Discovery of N -Hydroxyindole-Based Inhibitors of Human Lactate Dehydrogenase Isoform A (LDH-A) as Starvation Agents against Cancer Cells

2011 · Carlotta Granchi, Sarabindu Roy, et al. · Journal of Medicinal Chemistry · 227

Inhibitors of Lactate Dehydrogenase Isoforms and their Therapeutic Potentials

2010 · C. Granchi, S. Bertini, et al. · Current Medicinal Chemistry · 224

Inhibitors of histone deacetylase as antitumor agents: A critical review

2016 · Mohammed Manal, M.J.N. Chandrasekar, et al. · Bioorganic Chemistry · 216

Isoform-selective mechanism-based inhibition of human cytochrome P450 1A2 by furafylline

1993 · Kent L. Kunze, William F. Trager · Chemical Research in Toxicology · 216

Crystal structure of rofecoxib bound to human cyclooxygenase-2

2016 · Benjamin J. Orlando, Michael G. Malkowski · Acta Crystallographica Section F Structural Biology Communications · 203

PDF

Histone deacetylases: structural determinants of inhibitor selectivity

2015 · Carmina Micelli, Giulio Rastelli · Drug Discovery Today · 192

Sphingosine 1-phosphate and sphingosine kinases in health and disease: Recent advances

2016 · Susan Pyne, David R. Adams, et al. · Progress in Lipid Research · 189

PDF

Understanding the Selectivity of Genistein for Human Estrogen Receptor-β Using X-Ray Crystallography and Computational Methods

2004 · Eric S. Manas, Zhang B. Xu, et al. · Structure · 188

PDF

Aminoguanidine Is an Isoform-Selective, Mechanism-Based Inactivator of Nitric Oxide Synthase

1995 · D.J. Wolff, A. Lubeskie · Archives of Biochemistry and Biophysics · 187

Histone Deacetylase (HDAC) Inhibitors with a Novel Connecting Unit Linker Region Reveal a Selectivity Profile for HDAC4 and HDAC5 with Improved Activity against Chemoresistant Cancer Cells

2012 · Linda Marek, Alexandra Hamacher, et al. · Journal of Medicinal Chemistry · 177

Inhibitors of 17β-Hydroxysteroid Dehydrogenases

2003 · Donald Poirier · Current Medicinal Chemistry · 174

Works count: 1,101

Citation count: 29,750