Entry | Database: PDB / ID: 5ml0 |
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Title | Bromodomain of Mouse PCAF with (R)-4-chloro-2-methyl-5-((1-methylpiperidin-3-yl)amino)pyridazin-3(2H)-one |
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Components | Histone acetyltransferase KAT2B |
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Keywords | TRANSCRIPTION / INHIBITOR / HISTONE / EPIGENETIC READER / BROMODOMAIN / PCAF / ANTAGONIST |
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Function / homology | Function and homology information
: / : / : / : / B-WICH complex positively regulates rRNA expression / YAP1- and WWTR1 (TAZ)-stimulated gene expression / : / : / Regulation of FOXO transcriptional activity by acetylation / regulation of protein ADP-ribosylation ...: / : / : / : / B-WICH complex positively regulates rRNA expression / YAP1- and WWTR1 (TAZ)-stimulated gene expression / : / : / Regulation of FOXO transcriptional activity by acetylation / regulation of protein ADP-ribosylation / negative regulation of rRNA processing / Metalloprotease DUBs / NOTCH1 Intracellular Domain Regulates Transcription / RUNX3 regulates NOTCH signaling / Notch-HLH transcription pathway / diamine N-acetyltransferase / diamine N-acetyltransferase activity / negative regulation of centriole replication / peptidyl-lysine acetylation / RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function / lysine N-acetyltransferase activity, acting on acetyl phosphate as donor / Estrogen-dependent gene expression / actomyosin / internal peptidyl-lysine acetylation / negative regulation of cyclin-dependent protein serine/threonine kinase activity / cyclin-dependent protein serine/threonine kinase inhibitor activity / N-terminal peptidyl-lysine acetylation / I band / positive regulation of chromatin binding / limb development / A band / cell cycle / peptide-lysine-N-acetyltransferase activity / histone acetyltransferase binding / protein acetylation / acetyltransferase activity / transcription factor binding / histone acetyltransferase complex / histone acetyltransferase activity / histone acetyltransferase / positive regulation of gluconeogenesis / RNA polymerase II transcription regulatory region sequence-specific DNA binding / transcription coregulator activity / kinetochore / histone deacetylase binding / positive regulation of neuron projection development / cellular response to insulin stimulus / rhythmic process / heart development / transcription coactivator activity / chromatin remodeling / negative regulation of cell population proliferation / centrosome / chromatin binding / regulation of DNA-templated transcription / chromatin / protein kinase binding / positive regulation of DNA-templated transcription / positive regulation of transcription by RNA polymerase II / protein-containing complex / nucleoplasm / nucleus / cytosolSimilarity search - Function PCAF, N-terminal / Histone acetyltransferase GCN5/PCAF / PCAF (P300/CBP-associated factor) N-terminal domain / Histone acetyltransferase GCN5 / Acetyltransferase (GNAT) family / Gcn5-related N-acetyltransferase (GNAT) domain profile. / GNAT domain / Acyl-CoA N-acyltransferase / Bromodomain-like / Histone Acetyltransferase; Chain A ...PCAF, N-terminal / Histone acetyltransferase GCN5/PCAF / PCAF (P300/CBP-associated factor) N-terminal domain / Histone acetyltransferase GCN5 / Acetyltransferase (GNAT) family / Gcn5-related N-acetyltransferase (GNAT) domain profile. / GNAT domain / Acyl-CoA N-acyltransferase / Bromodomain-like / Histone Acetyltransferase; Chain A / Bromodomain, conserved site / Bromodomain signature. / Bromodomain / Bromodomain profile. / bromo domain / Bromodomain / Bromodomain-like superfamily / Up-down Bundle / Mainly AlphaSimilarity search - Domain/homology |
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Biological species | ![](img/tx_mammal.gif) Mus musculus (house mouse) |
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Method | X-RAY DIFFRACTION / MOLECULAR REPLACEMENT / Resolution: 1.64 Å |
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Authors | Chung, C.-W. |
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Citation | Journal: J. Med. Chem. / Year: 2017 Title: Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe. Authors: Humphreys, P.G. / Bamborough, P. / Chung, C.W. / Craggs, P.D. / Gordon, L. / Grandi, P. / Hayhow, T.G. / Hussain, J. / Jones, K.L. / Lindon, M. / Michon, A.M. / Renaux, J.F. / Suckling, C.J. ...Authors: Humphreys, P.G. / Bamborough, P. / Chung, C.W. / Craggs, P.D. / Gordon, L. / Grandi, P. / Hayhow, T.G. / Hussain, J. / Jones, K.L. / Lindon, M. / Michon, A.M. / Renaux, J.F. / Suckling, C.J. / Tough, D.F. / Prinjha, R.K. |
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History | Deposition | Dec 5, 2016 | Deposition site: PDBE / Processing site: PDBE |
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Revision 1.0 | Dec 20, 2017 | Provider: repository / Type: Initial release |
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Revision 1.1 | Jan 24, 2018 | Group: Database references / Category: citation / citation_author Item: _citation.country / _citation.journal_abbrev ..._citation.country / _citation.journal_abbrev / _citation.journal_id_ASTM / _citation.journal_id_CSD / _citation.journal_id_ISSN / _citation.journal_volume / _citation.page_first / _citation.page_last / _citation.pdbx_database_id_DOI / _citation.pdbx_database_id_PubMed / _citation.title / _citation.year |
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Revision 1.2 | May 8, 2024 | Group: Data collection / Database references / Category: chem_comp_atom / chem_comp_bond / database_2 Item: _database_2.pdbx_DOI / _database_2.pdbx_database_accession |
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