Demystifying Functional Parameters for Irreversible Enzyme Inhibitors
Covalent inhibitors (EGFR)
Tyrosine kinase
Covalent inhibitor kineticsSelectivity & kinome profiling
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More publications on Covalent
Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies
Zhai X, Ward RA, Doig P, Argyrou A · Biochemistry 2020
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR
Planken S, Behenna DC, Nair SK, … Lafontaine J · J Med Chem 2017
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants
Cheng H, Nair SK, Murray BW, … Kath JC · J Med Chem 2016
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway
Hagel M, Miduturu C, Sheets M, … Guzi T · Cancer Discov 2015
An algebraic model for the kinetics of covalent enzyme inhibition at low substrate concentrations
Kuzmič P, Solowiej J, Murray BW · Anal Biochem 2014
In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing
Tjin Tham Sjin R, Lee K, Walter AO, … Singh J · Mol Cancer Ther 2014
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