X-ray Crystal Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain

Summary for 2GQG
DescriptorProto-oncogene tyrosine-protein kinase ABL1, N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE, GLYCEROL, ... (4 entities in total)
Functional Keywordskinase, transferase
Biological sourceHomo sapiens (human)
Cellular locationCytoplasm, cytoskeleton. Isoform IB: Nucleus membrane; Lipid-anchor: P00519
Total number of polymer chains2
Total formula weight65503.58
Klei, H.E. (deposition date: 2006-04-20, release date: 2006-11-21, Last modification date: 2017-10-18)
Primary citationBorzilerri, R.,Chang, C.Y.J.,Cheng, J.D.,Kiefer, S.E.,Kish, K.,Klei, H.E.,Lee, F.Y.F.,Lombardo, L.J.,Newitt, J.,Tokarski, J.S.,Wittekind, M.,Xie, D.,Zhang, Y.
The Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain Elucidates Its Inhibitory Activity against Imatinib-Resistant ABL Mutants
CANCER RES., 66:5790-5797, 2006
PubMed: 16740718
DOI: 110.1158/0008-5472.CAN-05-4187
PDB entries with the same primary citation
Experimental method
Structure validation
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PDB entries from 2021-06-09