Entry Database : PDB / ID : 5amn Structure visualization Downloads & linksTitle The Discovery of 2-Substituted Phenol Quinazolines as Potent and Selective RET Kinase Inhibitors ComponentsPROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET Details Keywords TRANSFERASE / RET / ONCOGENE / RECEPTOR TYROSINE KINASE / CHEMICAL INHIBITOR / CANCERFunction / homology Function and homology informationFunction Domain/homology Component
Peyer's patch morphogenesis / positive regulation of metanephric glomerulus development / posterior midgut development / ureter maturation / embryonic epithelial tube formation / glial cell-derived neurotrophic factor receptor signaling pathway / lymphocyte migration into lymphoid organs / membrane protein proteolysis / positive regulation of peptidyl-serine phosphorylation of STAT protein / Formation of the ureteric bud ... Peyer's patch morphogenesis / positive regulation of metanephric glomerulus development / posterior midgut development / ureter maturation / embryonic epithelial tube formation / glial cell-derived neurotrophic factor receptor signaling pathway / lymphocyte migration into lymphoid organs / membrane protein proteolysis / positive regulation of peptidyl-serine phosphorylation of STAT protein / Formation of the ureteric bud / positive regulation of neuron maturation / Formation of the nephric duct / enteric nervous system development / neuron cell-cell adhesion / innervation / plasma membrane protein complex / neuron maturation / positive regulation of extrinsic apoptotic signaling pathway in absence of ligand / positive regulation of cell adhesion mediated by integrin / neural crest cell migration / ureteric bud development / response to pain / regulation of axonogenesis / homophilic cell adhesion via plasma membrane adhesion molecules / positive regulation of cell size / RET signaling / regulation of cell adhesion / cellular response to retinoic acid / NPAS4 regulates expression of target genes / transmembrane receptor protein tyrosine kinase activity / axon guidance / receptor protein-tyrosine kinase / positive regulation of neuron projection development / activation of cysteine-type endopeptidase activity involved in apoptotic process / MAPK cascade / retina development in camera-type eye / signaling receptor activity / RAF/MAP kinase cascade / protein tyrosine kinase activity / positive regulation of MAPK cascade / positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction / early endosome / receptor complex / endosome membrane / positive regulation of cell migration / response to xenobiotic stimulus / axon / protein phosphorylation / neuronal cell body / calcium ion binding / dendrite / positive regulation of gene expression / positive regulation of DNA-templated transcription / signal transduction / ATP binding / plasma membrane Similarity search - Function Tyrosine-protein kinase, Ret receptor / Tyrosine-protein kinase receptor Ret, cadherin like domain 3 / Ret, cadherin like domain 1 / RET, cadherin-like domain 4 / RET Cadherin like domain 1 / RET Cadherin like domain 3 / RET Cadherin like domain 4 / Cadherin domain / Cadherins domain profile. / Cadherin-like ... Tyrosine-protein kinase, Ret receptor / Tyrosine-protein kinase receptor Ret, cadherin like domain 3 / Ret, cadherin like domain 1 / RET, cadherin-like domain 4 / RET Cadherin like domain 1 / RET Cadherin like domain 3 / RET Cadherin like domain 4 / Cadherin domain / Cadherins domain profile. / Cadherin-like / Cadherin-like superfamily / Tyrosine-protein kinase, catalytic domain / Tyrosine kinase, catalytic domain / Tyrosine protein kinases specific active-site signature. / Tyrosine-protein kinase, active site / 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 / 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 / Resolution : 2.57 Å DetailsAuthors Newton, R. / Bowler, K. / Burns, E.M. / Chapman, P. / Fairweather, E. / Fritzl, S. / Goldberg, K. / Hamilton, N.M. / Holt, S.V. / Hopkins, G.V. ...Newton, R. / Bowler, K. / Burns, E.M. / Chapman, P. / Fairweather, E. / Fritzl, S. / Goldberg, K. / Hamilton, N.M. / Holt, S.V. / Hopkins, G.V. / Jones, S.D. / Jordan, A.M. / Lyons, A. / McDonald, N.Q. / Maguire, L.A. / Mould, D.P. / Purkiss, A.G. / Small, H.F. / Stowell, A. / Thomson, G.J. / Waddell, I.D. / Waszkowycz, B. / Watson, A.J. / Ogilvie, D.J. CitationJournal : Eur J Med Chem / Year : 2016Title : The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.Authors: Newton, R. / Bowler, K.A. / Burns, E.M. / Chapman, P.J. / Fairweather, E.E. / Fritzl, S.J.R. / Goldberg, K.M. / Hamilton, N.M. / Holt, S.V. / Hopkins, G.V. / Jones, S.D. / Jordan, A.M. / ... Authors : Newton, R. / Bowler, K.A. / Burns, E.M. / Chapman, P.J. / Fairweather, E.E. / Fritzl, S.J.R. / Goldberg, K.M. / Hamilton, N.M. / Holt, S.V. / Hopkins, G.V. / Jones, S.D. / Jordan, A.M. / Lyons, A.J. / Nikki March, H. / McDonald, N.Q. / Maguire, L.A. / Mould, D.P. / Purkiss, A.G. / Small, H.F. / Stowell, A.I.J. / Thomson, G.J. / Waddell, I.D. / Waszkowycz, B. / Watson, A.J. / Ogilvie, D.J. History Deposition Mar 11, 2015 Deposition site : PDBE / Processing site : PDBERevision 1.0 Feb 17, 2016 Provider : repository / Type : Initial releaseRevision 1.1 Mar 2, 2016 Group : Database referencesRevision 1.2 Feb 28, 2018 Group : Database references / Category : citation / citation_authorItem : _citation.journal_abbrev / _citation.journal_id_ISSN ... _citation.journal_abbrev / _citation.journal_id_ISSN / _citation.page_last / _citation.pdbx_database_id_DOI / _citation.title / _citation_author.name Revision 1.3 Jan 10, 2024 Group : Data collection / Database references ... Data collection / Database references / Derived calculations / Other / Refinement description Category : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_database_status / pdbx_initial_refinement_model / struct_conn / struct_site Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession ... _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_database_status.status_code_sf / _struct_conn.pdbx_leaving_atom_flag / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id
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