5XFJ

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

Summary for 5XFJ

• Entry DOI: 10.2210/pdb5xfj/pdb
• Related: 5XFF
• Descriptor: 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)
• Functional Keywords: inhibitor, kinase, gatekeeper, mutation, transferase
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 35167.45

Authors

Wu, D.,Chen, Y. (deposition date: 2017-04-10, release date: 2018-08-08, Last modification date: 2024-03-27)

Primary citation

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

Experimental method

X-RAY DIFFRACTION (3.25 Å)