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2GQG

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

Summary for 2GQG
Entry DOI10.2210/pdb2gqg/pdb
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
Authors
Klei, H.E. (deposition date: 2006-04-20, release date: 2006-11-21, Last modification date: 2017-10-18)
Primary citationTokarski, J.S.,Newitt, J.,Chang, C.Y.J.,Cheng, J.D.,Wittekind, M.,Kiefer, S.E.,Kish, K.,Lee, F.Y.F.,Borzilerri, R.,Lombardo, L.J.,Xie, D.,Zhang, Y.,Klei, H.E.
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
Cited by
PubMed: 16740718
DOI: 10.1158/0008-5472.CAN-05-4187
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.4 Å)
Structure validation

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