3IK3
AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance
Summary for 3IK3
Entry DOI | 10.2210/pdb3ik3/pdb |
Descriptor | Proto-oncogene tyrosine-protein kinase ABL1, 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam ide (3 entities in total) |
Functional Keywords | bcr-abl, cml, t315i, inhibitor, mutation, drug resistance, alternative splicing, atp-binding, cell adhesion, chromosomal rearrangement, cytoplasm, cytoskeleton, kinase, lipoprotein, magnesium, manganese, metal-binding, myristate, nucleotide-binding, nucleus, phosphoprotein, proto-oncogene, sh2 domain, sh3 domain, transferase |
Biological source | Mus musculus (mouse) |
Cellular location | Cytoplasm, cytoskeleton: P00520 |
Total number of polymer chains | 2 |
Total formula weight | 67573.16 |
Authors | Zhou, T. (deposition date: 2009-08-05, release date: 2009-11-03, Last modification date: 2023-09-06) |
Primary citation | O'Hare, T.,Shakespeare, W.C.,Zhu, X.,Eide, C.A.,Rivera, V.M.,Wang, F.,Adrian, L.T.,Zhou, T.,Huang, W.S.,Xu, Q.,Metcalf, C.A.,Tyner, J.W.,Loriaux, M.M.,Corbin, A.S.,Wardwell, S.,Ning, Y.,Keats, J.A.,Wang, Y.,Sundaramoorthi, R.,Thomas, M.,Zhou, D.,Snodgrass, J.,Commodore, L.,Sawyer, T.K.,Dalgarno, D.C.,Deininger, M.W.,Druker, B.J.,Clackson, T. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell, 16:401-412, 2009 Cited by PubMed: 19878872DOI: 10.1016/j.ccr.2009.09.028 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.9 Å) |
Structure validation
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