4RWK
Crystal structure of V561M FGFR1 gatekeeper mutation (C488A, C584S, V561M) in complex with N-{3-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-5-YL}-4-[(3R,5S)-3,5-DIMETHYLPIPERAZIN-1-YL]BENZAMIDE (AZD4547)
Summary for 4RWK
Entry DOI | 10.2210/pdb4rwk/pdb |
Related | 4RWI 4RWJ 4RWL |
Descriptor | Fibroblast growth factor receptor 1, N-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide, MAGNESIUM ION, ... (4 entities in total) |
Functional Keywords | receptor tyrosine kinase, gatekeeper mutation, proto-oncogene, kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Cell membrane; Single-pass type I membrane protein: P11362 |
Total number of polymer chains | 2 |
Total formula weight | 73468.78 |
Authors | Sohl, C.D.,Anderson, K.S. (deposition date: 2014-12-04, release date: 2015-04-15, Last modification date: 2023-09-20) |
Primary citation | Sohl, C.D.,Ryan, M.R.,Luo, B.,Frey, K.M.,Anderson, K.S. Illuminating the Molecular Mechanisms of Tyrosine Kinase Inhibitor Resistance for the FGFR1 Gatekeeper Mutation: The Achilles' Heel of Targeted Therapy. Acs Chem.Biol., 10:1319-1329, 2015 Cited by PubMed: 25686244DOI: 10.1021/acschembio.5b00014 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.982 Å) |
Structure validation
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