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TitleLY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance.
Journal, issue, pagesChem. Commun. (Camb. ), Vol. 54, Page 12089-12092, Year 2018
Publish dateApr 10, 2017 (structure data deposition date)
AuthorsWu, D. / Guo, M. / Min, X. / Dai, S. / Li, M. / Tan, S. / Li, G. / Chen, X. / Ma, Y. / Li, J. ...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.
External linksChem. Commun. (Camb. ) / PubMed:30298149
MethodsX-ray diffraction
Resolution2.7 - 3.25 Å
Structure data

PDB-5xff:
Crystal structure of LY2874455 in complex of FGFR4 gatekeeper mutation (V550L)
Method: X-RAY DIFFRACTION / Resolution: 2.7 Å

PDB-5xfj:
Crystal structure of LY2874455 in complex of FGFR4 gatekeeper mutation (V550M)
Method: X-RAY DIFFRACTION / Resolution: 3.25 Å

Chemicals

ChemComp-6LF:
2-[4-[E-2-[5-[(1R)-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / inhibitor / kinase / gatekeeper / mutation

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