5XFJ

Crystal structure of LY2874455 in complex of FGFR4 gatekeeper mutation (V550M)

5XFJ の概要

• エントリーDOI: 10.2210/pdb5xfj/pdb
• 関連するPDBエントリー: 5XFF
• 分子名称: Fibroblast growth factor receptor 4, 2-[4-[E-2-[5-[(1R)-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol (2 entities in total)
• 機能のキーワード: inhibitor, kinase, gatekeeper, mutation, transferase
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 35167.45

構造登録者

Wu, D.,Chen, Y. (登録日: 2017-04-10, 公開日: 2018-08-08, 最終更新日: 2024-03-27)

主引用文献

Wu, D.,Guo, M.,Min, X.,Dai, S.,Li, M.,Tan, S.,Li, G.,Chen, X.,Ma, Y.,Li, J.,Jiang, L.,Qu, L.,Zhou, Z.,Chen, Z.,Chen, L.,Xu, G.,Chen, Y.
LY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance.
Chem. Commun. (Camb.), 54:12089-12092, 2018

PubMed Abstract: The chemical compound LY2874455 has the potential to overcome drug resistance driven by FGFR gatekeeper mutations. X-ray crystallographic studies provide the structural explanation for why this compound is effective against the FGFR gatekeeper mutations.

PubMed: 30298149
DOI: 10.1039/c8cc07546h

実験手法

X-RAY DIFFRACTION (3.25 Å)