Entry Database : PDB / ID : 5qin Structure visualization Downloads & linksTitle TGF-BETA RECEPTOR TYPE 2 KINASE DOMAIN IN COMPLEX WITH N- {4-[3-(6-METHOXYPYRIDIN-3-YL)-1H-PYRROLO[3,2-B]PYRIDIN-2- YL]PYRIDIN-2-YL}ACETAMIDE ComponentsTGF-beta receptor type-2 Details Keywords TRANSFERASE/TRANSFERASE INHIBITOR / KINASE DOMAIN / TRANSFERASE-TRANSFERASE INHIBITOR COMPLEX / TRANSFERASEFunction / homology Function and homology informationFunction Domain/homology Component
positive regulation of tolerance induction to self antigen / positive regulation of B cell tolerance induction / inferior endocardial cushion morphogenesis / transforming growth factor beta receptor activity, type II / bronchus morphogenesis / mammary gland morphogenesis / lens fiber cell apoptotic process / growth plate cartilage chondrocyte growth / tricuspid valve morphogenesis / TGFBR2 MSI Frameshift Mutants in Cancer ... positive regulation of tolerance induction to self antigen / positive regulation of B cell tolerance induction / inferior endocardial cushion morphogenesis / transforming growth factor beta receptor activity, type II / bronchus morphogenesis / mammary gland morphogenesis / lens fiber cell apoptotic process / growth plate cartilage chondrocyte growth / tricuspid valve morphogenesis / TGFBR2 MSI Frameshift Mutants in Cancer / activin receptor activity / miRNA transport / type III transforming growth factor beta receptor binding / transforming growth factor beta ligand-receptor complex / Langerhans cell differentiation / aorta morphogenesis / positive regulation of epithelial to mesenchymal transition involved in endocardial cushion formation / TGFBR2 Kinase Domain Mutants in Cancer / transforming growth factor beta receptor activity / secondary palate development / cardiac left ventricle morphogenesis / SMAD2/3 Phosphorylation Motif Mutants in Cancer / TGFBR1 KD Mutants in Cancer / endocardial cushion fusion / positive regulation of T cell tolerance induction / membranous septum morphogenesis / lung lobe morphogenesis / positive regulation of NK T cell differentiation / regulation of stem cell proliferation / TGFBR1 LBD Mutants in Cancer / receptor protein serine/threonine kinase / transmembrane receptor protein serine/threonine kinase activity / activin binding / myeloid dendritic cell differentiation / type I transforming growth factor beta receptor binding / outflow tract septum morphogenesis / positive regulation of CD4-positive, alpha-beta T cell proliferation / SMAD protein signal transduction / regulation of stem cell differentiation / kinase activator activity / glycosaminoglycan binding / transforming growth factor beta binding / response to cholesterol / embryonic cranial skeleton morphogenesis / aortic valve morphogenesis / lens development in camera-type eye / atrioventricular valve morphogenesis / embryonic hemopoiesis / positive regulation of mesenchymal cell proliferation / artery morphogenesis / trachea formation / branching involved in blood vessel morphogenesis / smoothened signaling pathway / ventricular septum morphogenesis / activation of protein kinase activity / roof of mouth development / positive regulation of epithelial cell migration / blood vessel development / heart looping / outflow tract morphogenesis / TGF-beta receptor signaling activates SMADs / SMAD binding / positive regulation of SMAD protein signal transduction / epithelial to mesenchymal transition / vasculogenesis / positive regulation of epithelial to mesenchymal transition / gastrulation / Notch signaling pathway / transforming growth factor beta receptor signaling pathway / Downregulation of TGF-beta receptor signaling / TGF-beta receptor signaling in EMT (epithelial to mesenchymal transition) / caveola / brain development / cellular response to growth factor stimulus / positive regulation of angiogenesis / UCH proteinases / positive regulation of reactive oxygen species metabolic process / heart development / regulation of cell population proliferation / regulation of gene expression / in utero embryonic development / molecular adaptor activity / receptor complex / response to xenobiotic stimulus / membrane raft / external side of plasma membrane / positive regulation of cell population proliferation / apoptotic process / extracellular space / extracellular region / ATP binding / membrane / metal ion binding / plasma membrane / cytosol Similarity search - Function Transforming growth factor beta receptor 2 ectodomain / Transforming growth factor-beta receptor, type II / Transforming growth factor beta receptor 2 ectodomain / Ser/Thr protein kinase, TGFB receptor / Snake toxin-like superfamily / Protein tyrosine and serine/threonine kinase / Serine-threonine/tyrosine-protein kinase, catalytic domain / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 ... Transforming growth factor beta receptor 2 ectodomain / Transforming growth factor-beta receptor, type II / Transforming growth factor beta receptor 2 ectodomain / Ser/Thr protein kinase, TGFB receptor / Snake toxin-like superfamily / Protein tyrosine and serine/threonine kinase / Serine-threonine/tyrosine-protein kinase, catalytic domain / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Serine/threonine-protein kinase, active site / Serine/Threonine protein kinases active-site signature. / Serine/Threonine protein kinases, catalytic domain / 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 Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / molecular replacement / Resolution : 1.57 Å DetailsAuthors Sheriff, S. CitationJournal : ACS Med Chem Lett / Year : 2018Title : Discovery of 4-Azaindole Inhibitors of TGF beta RI as Immuno-oncology Agents.Authors: Zhang, Y. / Zhao, Y. / Tebben, A.J. / Sheriff, S. / Ruzanov, M. / Fereshteh, M.P. / Fan, Y. / Lippy, J. / Swanson, J. / Ho, C.P. / Wautlet, B.S. / Rose, A. / Parrish, K. / Yang, Z. / ... Authors : Zhang, Y. / Zhao, Y. / Tebben, A.J. / Sheriff, S. / Ruzanov, M. / Fereshteh, M.P. / Fan, Y. / Lippy, J. / Swanson, J. / Ho, C.P. / Wautlet, B.S. / Rose, A. / Parrish, K. / Yang, Z. / Donnell, A.F. / Zhang, L. / Fink, B.E. / Vite, G.D. / Augustine-Rauch, K. / Fargnoli, J. / Borzilleri, R.M. History Deposition Aug 5, 2018 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Oct 31, 2018 Provider : repository / Type : Initial releaseRevision 1.1 Dec 26, 2018 Group : Data collection / Database references / Category : citation / citation_authorItem : _citation.journal_abbrev / _citation.journal_volume ... _citation.journal_abbrev / _citation.journal_volume / _citation.page_first / _citation.page_last / _citation.pdbx_database_id_PubMed / _citation.title / _citation_author.name Revision 1.2 May 12, 2021 Group : Derived calculations / Structure summaryCategory : pdbx_deposit_group / pdbx_struct_conn_angle / struct_connItem : _pdbx_deposit_group.group_type / _pdbx_struct_conn_angle.ptnr1_auth_seq_id ... _pdbx_deposit_group.group_type / _pdbx_struct_conn_angle.ptnr1_auth_seq_id / _pdbx_struct_conn_angle.ptnr1_symmetry / _pdbx_struct_conn_angle.ptnr3_auth_seq_id / _pdbx_struct_conn_angle.ptnr3_symmetry / _pdbx_struct_conn_angle.value / _struct_conn.pdbx_dist_value / _struct_conn.ptnr2_auth_seq_id / _struct_conn.ptnr2_symmetry Revision 1.3 Mar 6, 2024 Group : Data collection / Database references / Category : chem_comp_atom / chem_comp_bond / database_2Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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