Entry Database : PDB / ID : 8g3c Structure visualization Downloads & linksTitle Crystal structure of human WDR5 in complex with N-[(2'-cyano[1,1'-biphenyl]-4-yl)methyl]-3-hydroxy-6-methyl-4-oxo-4H-pyran-2-carboxamide (compound 1, WDR5-MYC PPI inhibitor) ComponentsWD repeat-containing protein 5 Details Keywords ONCOPROTEIN/INHIBITOR / WDR5 / WBM / MYC / small molecule / ONCOPROTEIN-INHIBITOR complexFunction / homology Function and homology informationFunction Domain/homology Component
MLL3/4 complex / Set1C/COMPASS complex / MLL1/2 complex / ATAC complex / NSL complex / histone H3K4 methyltransferase activity / Cardiogenesis / histone methyltransferase complex / regulation of tubulin deacetylation / Formation of WDR5-containing histone-modifying complexes ... MLL3/4 complex / Set1C/COMPASS complex / MLL1/2 complex / ATAC complex / NSL complex / histone H3K4 methyltransferase activity / Cardiogenesis / histone methyltransferase complex / regulation of tubulin deacetylation / Formation of WDR5-containing histone-modifying complexes / regulation of cell division / regulation of embryonic development / MLL1 complex / transcription factor TFIID complex / RNA polymerase II general transcription initiation factor activity / histone acetyltransferase complex / positive regulation of gluconeogenesis / transcription initiation-coupled chromatin remodeling / methylated histone binding / skeletal system development / gluconeogenesis / RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function / mitotic spindle / PKMTs methylate histone lysines / RMTs methylate histone arginines / Activation of anterior HOX genes in hindbrain development during early embryogenesis / Neddylation / HATs acetylate histones / histone binding / regulation of cell cycle / regulation of DNA-templated transcription / regulation of transcription by RNA polymerase II / positive regulation of DNA-templated transcription / negative regulation of transcription by RNA polymerase II / nucleoplasm / nucleus Similarity search - Function G-protein beta WD-40 repeat / WD40 repeat, conserved site / Trp-Asp (WD) repeats signature. / Trp-Asp (WD) repeats profile. / Trp-Asp (WD) repeats circular profile. / WD domain, G-beta repeat / WD40 repeats / WD40 repeat / WD40-repeat-containing domain superfamily / WD40/YVTN repeat-like-containing domain superfamily Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 1.8 Å DetailsAuthors Zhao, M. Funding support 1items Details Hide detailsOrganization Grant number Country Not funded
CitationJournal : J.Med.Chem. / Year : 2023Title : Discovery and Structure-Based Design of Inhibitors of the WD Repeat-Containing Protein 5 (WDR5)-MYC Interaction.Authors: Ding, J. / Liu, L. / Chiang, Y.L. / Zhao, M. / Liu, H. / Yang, F. / Shen, L. / Lin, Y. / Deng, H. / Gao, J. / Sage, D.R. / West, L. / Llamas, L.A. / Hao, X. / Kawatkar, S. / Li, E. / Jain, R. ... Authors : Ding, J. / Liu, L. / Chiang, Y.L. / Zhao, M. / Liu, H. / Yang, F. / Shen, L. / Lin, Y. / Deng, H. / Gao, J. / Sage, D.R. / West, L. / Llamas, L.A. / Hao, X. / Kawatkar, S. / Li, E. / Jain, R.K. / Tallarico, J.A. / Canham, S.M. / Wang, H. History Deposition Feb 7, 2023 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Jun 28, 2023 Provider : repository / Type : Initial releaseRevision 1.1 Jul 5, 2023 Group : Database references / Category : citation / citation_authorItem : _citation.journal_volume / _citation.page_first ... _citation.journal_volume / _citation.page_first / _citation.page_last / _citation_author.identifier_ORCID Revision 1.2 Oct 25, 2023 Group : Data collection / Refinement descriptionCategory : chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_modelItem : _pdbx_initial_refinement_model.details
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