2GQG
X-ray Crystal Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain
Summary for 2GQG
Entry DOI | 10.2210/pdb2gqg/pdb |
Descriptor | Proto-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 Keywords | kinase, transferase |
Biological source | Homo sapiens (human) |
Cellular location | Cytoplasm, cytoskeleton. Isoform IB: Nucleus membrane; Lipid-anchor: P00519 |
Total number of polymer chains | 2 |
Total formula weight | 65503.58 |
Authors | Klei, H.E. (deposition date: 2006-04-20, release date: 2006-11-21, Last modification date: 2017-10-18) |
Primary citation | Tokarski, 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: 16740718DOI: 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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