Entry | Database: PDB / ID: 4c67 |
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Title | Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains |
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Components | BROMODOMAIN-CONTAINING PROTEIN 4 |
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Keywords | CELL CYCLE / HISTONE / EPIGENETIC READER BRD4 / BROMODOMAIN CONTAINING PROTEIN 4 / ANTAGONIST |
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Function / homology | Function and homology information
RNA polymerase II C-terminal domain binding / negative regulation of DNA damage checkpoint / P-TEFb complex binding / negative regulation by host of viral transcription / positive regulation of T-helper 17 cell lineage commitment / positive regulation of G2/M transition of mitotic cell cycle / histone reader activity / RNA polymerase II CTD heptapeptide repeat kinase activity / condensed nuclear chromosome / positive regulation of transcription elongation by RNA polymerase II ...RNA polymerase II C-terminal domain binding / negative regulation of DNA damage checkpoint / P-TEFb complex binding / negative regulation by host of viral transcription / positive regulation of T-helper 17 cell lineage commitment / positive regulation of G2/M transition of mitotic cell cycle / histone reader activity / RNA polymerase II CTD heptapeptide repeat kinase activity / condensed nuclear chromosome / positive regulation of transcription elongation by RNA polymerase II / transcription coregulator activity / lysine-acetylated histone binding / p53 binding / chromosome / regulation of inflammatory response / positive regulation of canonical NF-kappaB signal transduction / Potential therapeutics for SARS / transcription coactivator activity / transcription cis-regulatory region binding / chromatin remodeling / DNA damage response / chromatin binding / regulation of transcription by RNA polymerase II / positive regulation of DNA-templated transcription / enzyme binding / positive regulation of transcription by RNA polymerase II / nucleoplasm / nucleusSimilarity search - Function Bromodomain protein 4, C-terminal / C-terminal domain of bromodomain protein 4 / NET domain superfamily / NET domain profile. / Brdt, bromodomain, repeat II / : / Brdt, bromodomain, repeat I / NET domain / Bromodomain extra-terminal - transcription regulation / Bromodomain-like ...Bromodomain protein 4, C-terminal / C-terminal domain of bromodomain protein 4 / NET domain superfamily / NET domain profile. / Brdt, bromodomain, repeat II / : / Brdt, bromodomain, repeat I / NET domain / Bromodomain extra-terminal - transcription regulation / 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 | HOMO SAPIENS (human) |
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Method | X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution: 1.55 Å |
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Authors | Chung, C. / Mirguet, O. |
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Citation | Journal: J.Med.Chem. / Year: 2013 Title: Discovery of Epigenetic Regulator I-Bet762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the Bet Bromodomains. Authors: Mirguet, O. / Gosmini, R. / Toum, J. / Clement, C. / Barnathan, M. / Brusq, J. / Mordaunt, J.E. / Grimes, R. / Crowe, M. / Pineau, O. / Ajakane, M. / Daugan, A. / Jeffrey, P. / Cutler, L. / ...Authors: Mirguet, O. / Gosmini, R. / Toum, J. / Clement, C. / Barnathan, M. / Brusq, J. / Mordaunt, J.E. / Grimes, R. / Crowe, M. / Pineau, O. / Ajakane, M. / Daugan, A. / Jeffrey, P. / Cutler, L. / Haynes, A. / Smithers, N. / Chung, C. / Bamborough, P. / Uings, I.J. / Lewis, T. / Witherington, J. / Parr, N. / Prinjha, R. / Nicodeme, E. |
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History | Deposition | Sep 17, 2013 | Deposition site: PDBE / Processing site: PDBE |
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Revision 1.0 | Oct 2, 2013 | Provider: repository / Type: Initial release |
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Revision 1.1 | Oct 30, 2013 | Group: Database references |
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Revision 1.2 | May 8, 2024 | Group: Data collection / Database references ...Data collection / Database references / Derived calculations / Other Category: chem_comp_atom / chem_comp_bond ...chem_comp_atom / chem_comp_bond / database_2 / pdbx_database_status / 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_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id |
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