Entry | Database: PDB / ID: 4uyh |
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Title | N-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 1-((2R,4S)-2-methyl-4-(phenylamino)-6-(4-(piperidin-1-ylmethyl)phenyl)-3,4-dihydroquinolin-1(2H)-yl)ethanone |
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Components | BROMODOMAIN-CONTAINING PROTEIN 2 |
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Keywords | TRANSCRIPTION / HISTONE / EPIGENETIC READER / BET / BRD2 / BROMODOMAIN |
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Function / homology | Function and homology information
acetylation-dependent protein binding / chromatin looping / RUNX3 regulates p14-ARF / positive regulation of T-helper 17 cell lineage commitment / protein localization to chromatin / neural tube closure / lysine-acetylated histone binding / nucleosome assembly / spermatogenesis / nuclear speck ...acetylation-dependent protein binding / chromatin looping / RUNX3 regulates p14-ARF / positive regulation of T-helper 17 cell lineage commitment / protein localization to chromatin / neural tube closure / lysine-acetylated histone binding / nucleosome assembly / spermatogenesis / nuclear speck / protein serine/threonine kinase activity / chromatin binding / chromatin / regulation of transcription by RNA polymerase II / 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 / 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 / MOLECULAR REPLACEMENT / Resolution: 1.73 Å |
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Authors | Chung, C. / Bamborough, P. / Gosmini, R. |
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Citation | Journal: J.Med.Chem. / Year: 2014 Title: The Discovery of I-Bet726 (Gsk1324726A), a Potent Tetrahydroquinoline Apoa1 Up-Regulator and Selective Bet Bromodomain Inhibitor. Authors: Gosmini, R. / Nguyen, V.L. / Toum, J. / Simon, C. / Brusq, J.M. / Krysa, G. / Mirguet, O. / Riou-Eymard, A.M. / Boursier, E.V. / Trottet, L. / Bamborough, P. / Clark, H. / Chung, C.W. / ...Authors: Gosmini, R. / Nguyen, V.L. / Toum, J. / Simon, C. / Brusq, J.M. / Krysa, G. / Mirguet, O. / Riou-Eymard, A.M. / Boursier, E.V. / Trottet, L. / Bamborough, P. / Clark, H. / Chung, C.W. / Cutler, L. / Demont, E.H. / Kaur, R. / Lewis, A.J. / Schilling, M.B. / Soden, P.E. / Taylor, S. / Walker, A.L. / Walker, M.D. / Prinjha, R.K. / Nicodeme, E. |
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History | Deposition | Aug 31, 2014 | Deposition site: PDBE / Processing site: PDBE |
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Revision 1.0 | Oct 8, 2014 | Provider: repository / Type: Initial release |
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Revision 1.1 | Oct 22, 2014 | Group: Database references |
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Revision 1.2 | May 15, 2019 | Group: Data collection / Experimental preparation / Other Category: exptl_crystal_grow / pdbx_database_proc / pdbx_database_status Item: _exptl_crystal_grow.temp / _pdbx_database_status.recvd_author_approval |
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Revision 1.3 | 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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