Entry Database : PDB / ID : 4x2i Structure visualization Downloads & linksTitle Discovery of benzotriazolo diazepines as orally-active inhibitors of BET bromodomains: Crystal structure of BRD4 with CPI-13 ComponentsBromodomain-containing protein 4 Details Keywords SIGNALING PROTEIN / BET / CPI-13Function / homology Function and homology informationFunction Domain/homology Component
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 / nucleus Similarity 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 Alpha Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 1.2 Å DetailsAuthors Bellon, S.F. / Jayaram, H. / Poy, F. CitationJournal : Acs Med.Chem.Lett. / Year : 2016Title : Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.Authors: Taylor, A.M. / Vaswani, R.G. / Gehling, V.S. / Hewitt, M.C. / Leblanc, Y. / Audia, J.E. / Bellon, S. / Cummings, R.T. / Cote, A. / Harmange, J.C. / Jayaram, H. / Joshi, S. / Lora, J.M. / ... Authors : Taylor, A.M. / Vaswani, R.G. / Gehling, V.S. / Hewitt, M.C. / Leblanc, Y. / Audia, J.E. / Bellon, S. / Cummings, R.T. / Cote, A. / Harmange, J.C. / Jayaram, H. / Joshi, S. / Lora, J.M. / Mertz, J.A. / Neiss, A. / Pardo, E. / Nasveschuk, C.G. / Poy, F. / Sandy, P. / Setser, J.W. / Sims, R.J. / Tang, Y. / Albrecht, B.K. History Deposition Nov 26, 2014 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Nov 11, 2015 Provider : repository / Type : Initial releaseRevision 1.1 Mar 30, 2016 Group : Database referencesRevision 1.2 Feb 28, 2024 Group : Data collection / Database references / Derived calculationsCategory : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_struct_oper_list Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_struct_oper_list.symmetry_operation
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