TAS‐120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure

• Published in: ChemMedChem Vol. 14; no. 4; pp. 494 - 500
• Main Authors: Kalyukina, Maria, Yosaatmadja, Yuliana, Middleditch, Martin J., Patterson, Adam V., Smaill, Jeff B., Squire, Christopher J.
• Format: Journal Article
• Language: English
• Published: Germany Wiley Subscription Services, Inc 19.02.2019
• Subjects: Acrylamide; Cancer; Chemical reactions; Clinical trials; conformational sampling; Coordination compounds; Covalence; Crystal structure; drug discovery; Fast chemical reactions; fibroblast growth factor receptor; Fibroblast growth factor receptor 1; Fibroblast growth factor receptors; Fibroblasts; Growth factors; Inhibitors; irreversible inhibitor; Kinases; Mass spectrometry; Mass spectroscopy; Medical research; Metastases; Organic chemistry; Protein-tyrosine kinase; Proteins; Reactivity; Solid tumors; TAS-120; Tumors; Tyrosine; irreversible inhibitor; conformational sampling; drug discovery; TAS-120; fibroblast growth factor receptor

1‐[(3S)‐3‐[4‐Amino‐3‐[2‐(3,5‐dimethoxyphenyl)ethynyl]‐1H‐pyrazolo[3,4‐d]pyrimidin‐1‐yl]‐1‐pyrrolidinyl]‐2‐propen‐1‐one (TAS‐120) is an irreversible inhibitor of the fibroblast growth factor receptor (FGFR) family, and is currently under phase I/II clinical trials in patients with confirmed advanced...