3G0F

KIT kinase domain mutant D816H in complex with sunitinib

Summary for 3G0F

• Entry DOI: 10.2210/pdb3g0f/pdb
• Related: 3G0E
• Descriptor: Mast/stem cell growth factor receptor, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo xamide, SULFATE ION, ... (4 entities in total)
• Functional Keywords: kit kinase domain, sutent binding, drug resistance, atp-binding, disease mutation, glycoprotein, immunoglobulin domain, kinase, membrane, nucleotide-binding, phosphoprotein, polymorphism, proto-oncogene, receptor, transmembrane, tyrosine-protein kinase, transferase
• Biological source: Homo sapiens (human); More
• Cellular location: Isoform 1: Cell membrane; Single-pass type I membrane protein. Isoform 2: Cell membrane; Single-pass type I membrane protein. Isoform 3: Cytoplasm: P10721
• Total number of polymer chains: 2
• Total formula weight: 77373.49

Authors

Gajiwala, K.S.,Wu, J.C.,Lunney, E.A.,Demetri, G.D. (deposition date: 2009-01-27, release date: 2009-02-24, Last modification date: 2024-04-03)

• Primary citation: Gajiwala, K.S.,Wu, J.C.,Christensen, J.,Deshmukh, G.D.,Diehl, W.,DiNitto, J.P.,English, J.M.,Greig, M.J.,He, Y.A.,Jacques, S.L.,Lunney, E.A.,McTigue, M.,Molina, D.,Quenzer, T.,Wells, P.A.,Yu, X.,Zhang, Y.,Zou, A.,Emmett, M.R.,Marshall, A.G.,Zhang, H.M.,Demetri, G.D.; KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.; Proc.Natl.Acad.Sci.USA, 106:1542-1547, 2009; PubMed: 19164557; DOI: 10.1073/pnas.0812413106

Experimental method

X-RAY DIFFRACTION (2.6 Å)