Entry Database : PDB / ID : 3ik3 Structure visualization Downloads & linksTitle AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance ComponentsProto-oncogene tyrosine-protein kinase ABL1 Details Keywords TRANSFERASE / 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 domainFunction / homology Function and homology informationFunction Domain/homology Component
Role of ABL in ROBO-SLIT signaling / HDR through Single Strand Annealing (SSA) / RHO GTPases Activate WASPs and WAVEs / Cyclin D associated events in G1 / Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks / protein localization to cytoplasmic microtubule plus-end / DN4 thymocyte differentiation / response to epinephrine / regulation of cellular senescence / podocyte apoptotic process ... Role of ABL in ROBO-SLIT signaling / HDR through Single Strand Annealing (SSA) / RHO GTPases Activate WASPs and WAVEs / Cyclin D associated events in G1 / Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks / protein localization to cytoplasmic microtubule plus-end / DN4 thymocyte differentiation / response to epinephrine / regulation of cellular senescence / podocyte apoptotic process / RUNX1 regulates transcription of genes involved in differentiation of HSCs / transitional one stage B cell differentiation / DNA conformation change / circulatory system development / regulation of modification of synaptic structure / Regulation of actin dynamics for phagocytic cup formation / delta-catenin binding / positive regulation of extracellular matrix organization / B cell proliferation involved in immune response / neuroepithelial cell differentiation / microspike assembly / positive regulation of Wnt signaling pathway, planar cell polarity pathway / cerebellum morphogenesis / regulation of extracellular matrix organization / positive regulation of blood vessel branching / B-1 B cell homeostasis / neuropilin signaling pathway / neuropilin binding / bubble DNA binding / Myogenesis / activated T cell proliferation / proline-rich region binding / regulation of Cdc42 protein signal transduction / mitogen-activated protein kinase binding / positive regulation of dendrite development / myoblast proliferation / syntaxin binding / alpha-beta T cell differentiation / cardiac muscle cell proliferation / regulation of T cell differentiation / regulation of axon extension / positive regulation of cell migration involved in sprouting angiogenesis / negative regulation of cell-cell adhesion / B cell proliferation / cell leading edge / positive regulation of osteoblast proliferation / regulation of microtubule polymerization / platelet-derived growth factor receptor-beta signaling pathway / negative regulation of cellular senescence / positive regulation of focal adhesion assembly / associative learning / Bergmann glial cell differentiation / platelet-derived growth factor receptor signaling pathway / neuromuscular process controlling balance / negative regulation of mitotic cell cycle / negative regulation of long-term synaptic potentiation / negative regulation of BMP signaling pathway / negative regulation of double-strand break repair via homologous recombination / endothelial cell migration / signal transduction in response to DNA damage / positive regulation of T cell migration / BMP signaling pathway / negative regulation of endothelial cell apoptotic process / canonical NF-kappaB signal transduction / phagocytosis / positive regulation of substrate adhesion-dependent cell spreading / four-way junction DNA binding / spleen development / positive regulation of vasoconstriction / cellular response to transforming growth factor beta stimulus / positive regulation of stress fiber assembly / ruffle / response to endoplasmic reticulum stress / positive regulation of establishment of T cell polarity / phosphotyrosine residue binding / ephrin receptor binding / positive regulation of interleukin-2 production / ERK1 and ERK2 cascade / actin filament polymerization / SH2 domain binding / post-embryonic development / positive regulation of mitotic cell cycle / substrate adhesion-dependent cell spreading / thymus development / positive regulation of release of sequestered calcium ion into cytosol / integrin-mediated signaling pathway / establishment of localization in cell / neural tube closure / regulation of actin cytoskeleton organization / non-specific protein-tyrosine kinase / protein kinase C binding / B cell receptor signaling pathway / non-membrane spanning protein tyrosine kinase activity / epidermal growth factor receptor signaling pathway / neuron differentiation / negative regulation of ERK1 and ERK2 cascade / peptidyl-tyrosine phosphorylation / SH3 domain binding / cell-cell adhesion / autophagy Similarity search - Function F-actin binding / F-actin binding / F-actin binding domain (FABD) / Tyrosine-protein kinase ABL, SH2 domain / : / SH3 domain / SH2 domain / Src homology 2 (SH2) domain profile. / Src homology 2 domains / SH2 domain ... F-actin binding / F-actin binding / F-actin binding domain (FABD) / Tyrosine-protein kinase ABL, SH2 domain / : / SH3 domain / SH2 domain / Src homology 2 (SH2) domain profile. / Src homology 2 domains / SH2 domain / Src homology 3 domains / SH2 domain superfamily / SH3-like domain superfamily / Src homology 3 (SH3) domain profile. / SH3 domain / Tyrosine-protein kinase, catalytic domain / Tyrosine kinase, catalytic domain / Tyrosine protein kinases specific active-site signature. / Tyrosine-protein kinase, active site / Serine-threonine/tyrosine-protein kinase, catalytic domain / Protein tyrosine and serine/threonine kinase / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Protein kinase, ATP binding site / Protein kinases ATP-binding region signature. / Protein kinase domain profile. / Protein kinase domain / Protein kinase-like domain superfamily / 2-Layer Sandwich / Orthogonal Bundle / Mainly Alpha / Alpha Beta Similarity search - Domain/homologyBiological species Mus musculus (house mouse)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 1.9 Å DetailsAuthors Zhou, T. CitationJournal : Cancer Cell / Year : 2009Title : AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.Authors: 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. ... Authors : 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. History Deposition Aug 5, 2009 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Nov 3, 2009 Provider : repository / Type : Initial releaseRevision 1.1 Jul 13, 2011 Group : Version format complianceRevision 1.2 Oct 13, 2021 Group : Database references / Derived calculations / Structure summaryCategory : chem_comp / database_2 ... chem_comp / database_2 / entity / pdbx_entity_nonpoly / struct_ref_seq_dif / struct_site Item : _chem_comp.name / _database_2.pdbx_DOI ... _chem_comp.name / _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _entity.pdbx_description / _pdbx_entity_nonpoly.name / _struct_ref_seq_dif.details / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id Revision 1.3 Sep 6, 2023 Group : Data collection / Refinement descriptionCategory : chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_model
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