8E1X

FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29)

8E1X の概要

• エントリーDOI: 10.2210/pdb8e1x/pdb
• 分子名称: Fibroblast growth factor receptor 2, (5M)-N-methyl-5-{(6M,8S)-5-{[(3S)-oxolan-3-yl]amino}-6-[1-(propan-2-yl)-1H-pyrazol-3-yl]pyrazolo[1,5-a]pyrimidin-3-yl}pyridine-3-carboxamide (3 entities in total)
• 機能のキーワード: fgfr, inhibitor, kinase, gatekeeper, hyperphosphatemia, structural protein
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 76539.42

構造登録者

Lei, H.-T.,Epling, L.B.,Deller, M.C. (登録日: 2022-08-11, 公開日: 2022-11-23, 最終更新日: 2023-11-15)

• 主引用文献: Shvartsbart, A.,Roach, J.J.,Witten, M.R.,Koblish, H.,Harris, J.J.,Covington, M.,Hess, R.,Lin, L.,Frascella, M.,Truong, L.,Leffet, L.,Conlen, P.,Beshad, E.,Klabe, R.,Katiyar, K.,Kaldon, L.,Young-Sciame, R.,He, X.,Petusky, S.,Chen, K.J.,Horsey, A.,Lei, H.T.,Epling, L.B.,Deller, M.C.,Vechorkin, O.,Yao, W.; Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.; J.Med.Chem., 65:15433-15442, 2022; PubMed: 36356320; DOI: 10.1021/acs.jmedchem.2c01366

実験手法

X-RAY DIFFRACTION (2.68 Å)