Entry | Database: PDB / ID: 5ek9 |
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Title | Crystal structure of the second bromodomain of human BRD2 in complex with a tetrahydroquinoline inhibitor |
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Components | Bromodomain-containing protein 2 |
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Keywords | TRANSCRIPTION / chromatin and transcription regulator / acetylation / Structural Genomics / Structural Genomics Consortium / SGC |
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Function / homology | Function and homology information
acetylation-dependent protein binding / chromatin looping / positive regulation of T-helper 17 cell lineage commitment / RUNX3 regulates p14-ARF / protein localization to chromatin / lysine-acetylated histone binding / neural tube closure / nucleosome assembly / spermatogenesis / nuclear speck ...acetylation-dependent protein binding / chromatin looping / positive regulation of T-helper 17 cell lineage commitment / RUNX3 regulates p14-ARF / protein localization to chromatin / lysine-acetylated histone binding / neural tube closure / nucleosome assembly / spermatogenesis / nuclear speck / protein serine/threonine kinase activity / chromatin binding / regulation of transcription by RNA polymerase II / chromatin / nucleoplasm / nucleus / cytoplasmSimilarity search - Function 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 ...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 profile. / bromo domain / Bromodomain / Bromodomain-like superfamily / Bromodomain / 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: 2.08 Å |
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Authors | Tallant, C. / Slavish, P.J. / Siejka, P. / Bharatham, N. / Shadrick, W.R. / Chai, S. / Young, B.M. / Boyd, V.A. / Heroven, C. / Picaud, S. ...Tallant, C. / Slavish, P.J. / Siejka, P. / Bharatham, N. / Shadrick, W.R. / Chai, S. / Young, B.M. / Boyd, V.A. / Heroven, C. / Picaud, S. / Fedorov, O. / Chen, T. / Lee, R.E. / Guy, R.K. / Shelat, A.A. / von Delft, F. / Arrowsmith, C.H. / Edwards, A.M. / Bountra, C. / Knapp, S. / Structural Genomics Consortium (SGC) |
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Citation | Journal: Bioorg. Med. Chem. / Year: 2018 Title: Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. Authors: Shadrick, W.R. / Slavish, P.J. / Chai, S.C. / Waddell, B. / Connelly, M. / Low, J.A. / Tallant, C. / Young, B.M. / Bharatham, N. / Knapp, S. / Boyd, V.A. / Morfouace, M. / Roussel, M.F. / ...Authors: Shadrick, W.R. / Slavish, P.J. / Chai, S.C. / Waddell, B. / Connelly, M. / Low, J.A. / Tallant, C. / Young, B.M. / Bharatham, N. / Knapp, S. / Boyd, V.A. / Morfouace, M. / Roussel, M.F. / Chen, T. / Lee, R.E. / Kiplin Guy, R. / Shelat, A.A. / Potter, P.M. |
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History | Deposition | Nov 3, 2015 | Deposition site: RCSB / Processing site: PDBE |
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Revision 1.0 | Nov 16, 2016 | Provider: repository / Type: Initial release |
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Revision 1.1 | Nov 29, 2017 | 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.pdbx_database_id_DOI / _citation.title / _citation.year |
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Revision 1.2 | Dec 13, 2017 | Group: Database references / Category: citation / citation_author Item: _citation.journal_abbrev / _citation.pdbx_database_id_PubMed ..._citation.journal_abbrev / _citation.pdbx_database_id_PubMed / _citation.title / _citation_author.name |
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Revision 1.3 | Jan 17, 2018 | Group: Database references / Category: citation Item: _citation.journal_volume / _citation.page_first ..._citation.journal_volume / _citation.page_first / _citation.page_last / _citation.year |
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Revision 1.4 | 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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