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: 25686244 DOI: 10.1021/acschembio.5b00014 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.982 Å)

Structure validation