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Structure paper

TitleA novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.
Journal, issue, pagesJ. Biol. Chem., Vol. 286, Page 20677-20687, Year 2011
Publish dateApr 12, 2011 (structure data deposition date)
AuthorsEathiraj, S. / Palma, R. / Hirschi, M. / Volckova, E. / Nakuci, E. / Castro, J. / Chen, C.R. / Chan, T.C. / France, D.S. / Ashwell, M.A.
External linksJ. Biol. Chem. / PubMed:21454610
MethodsX-ray diffraction
Resolution2.01 - 2.1 Å
Structure data

PDB-3rhx:
Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069
Method: X-RAY DIFFRACTION / Resolution: 2.01 Å

PDB-3ri1:
Crystal structure of the catalytic domain of FGFR2 kinase in complex with ARQ 069
Method: X-RAY DIFFRACTION / Resolution: 2.1 Å

Chemicals

ChemComp-3RH:
(6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine

ChemComp-SO4:
SULFATE ION

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / FGFR1 kinase / FGFR2 kinase / inactive conformation / kinase-inhibitor complex / TRANSFERASE-TRANSFERASE INHIBITOR complex

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