Entry Database : PDB / ID : 5a2s Structure visualization Downloads & linksTitle Potent, selective and CNS-penetrant tetrasubstituted cyclopropane class IIa histone deacetylase (HDAC) inhibitors ComponentsHISTONE DEACETYLASE 4 Details Keywords HYDROLASE / CLASS IIA HDAC INHIBITORS / HYDROXAMIC ACID / CNS EXPOSURE / TETRASUBSTITUTED CYCLOPROPANE / CYCLOPROPANATION / HUNTINGTON'S DISEASEFunction / homology Function and homology informationFunction Domain/homology Component
RUNX2 regulates chondrocyte maturation / response to denervation involved in regulation of muscle adaptation / negative regulation of myotube differentiation / peptidyl-lysine deacetylation / positive regulation of protein sumoylation / regulation of protein binding / negative regulation of transcription by competitive promoter binding / protein deacetylation / cardiac muscle hypertrophy in response to stress / histone deacetylase ... RUNX2 regulates chondrocyte maturation / response to denervation involved in regulation of muscle adaptation / negative regulation of myotube differentiation / peptidyl-lysine deacetylation / positive regulation of protein sumoylation / regulation of protein binding / negative regulation of transcription by competitive promoter binding / protein deacetylation / cardiac muscle hypertrophy in response to stress / histone deacetylase / protein lysine deacetylase activity / negative regulation of glycolytic process / SUMO transferase activity / negative regulation of gene expression, epigenetic / histone deacetylase activity / type I interferon-mediated signaling pathway / B cell activation / Notch-HLH transcription pathway / potassium ion binding / RUNX3 regulates p14-ARF / histone deacetylase complex / protein sumoylation / transcription repressor complex / SUMOylation of chromatin organization proteins / response to interleukin-1 / B cell differentiation / SUMOylation of intracellular receptors / negative regulation of DNA-binding transcription factor activity / NOTCH1 Intracellular Domain Regulates Transcription / Constitutive Signaling by NOTCH1 PEST Domain Mutants / Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants / positive regulation of DNA-binding transcription factor activity / histone deacetylase binding / nervous system development / DNA-binding transcription factor binding / RNA polymerase II-specific DNA-binding transcription factor binding / molecular adaptor activity / nuclear speck / chromatin remodeling / inflammatory response / RNA polymerase II cis-regulatory region sequence-specific DNA binding / positive regulation of cell population proliferation / chromatin / positive regulation of DNA-templated transcription / negative regulation of transcription by RNA polymerase II / positive regulation of transcription by RNA polymerase II / zinc ion binding / nucleoplasm / identical protein binding / nucleus / cytoplasm / cytosol Similarity search - Function Histone deacetylase, glutamine rich N-terminal domain / Glutamine rich N terminal domain of histone deacetylase 4 / : / Histone deacetylase domain / Arginase; Chain A / Histone deacetylase family / Histone deacetylase domain / Histone deacetylase domain superfamily / Histone deacetylase domain / Ureohydrolase domain superfamily ... Histone deacetylase, glutamine rich N-terminal domain / Glutamine rich N terminal domain of histone deacetylase 4 / : / Histone deacetylase domain / Arginase; Chain A / Histone deacetylase family / Histone deacetylase domain / Histone deacetylase domain superfamily / Histone deacetylase domain / Ureohydrolase domain superfamily / 3-Layer(aba) Sandwich / Alpha Beta Similarity search - Domain/homologyBiological species HOMO SAPIENS (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 2.65 Å DetailsAuthors Luckhurst, C.A. / Breccia, P. / Stott, A.J. / Aziz, O. / Birch, H. / Burli, R.W. / Hughes, S. / Jarvis, R.E. / Lamers, M. / Leonard, P. ...Luckhurst, C.A. / Breccia, P. / Stott, A.J. / Aziz, O. / Birch, H. / Burli, R.W. / Hughes, S. / Jarvis, R.E. / Lamers, M. / Leonard, P. / Matthews, K.L. / McAllister, G. / Pollack, S. / Saville-Stones, E. / Wishart, G. / Yates, D. / Dominguez, C. CitationJournal : Acs Med.Chem.Lett. / Year : 2016Title : Potent, Selective, and Cns-Penetrant Tetrasubstituted Cyclopropane Class Iia Histone Deacetylase (Hdac) Inhibitors.Authors: Luckhurst, C.A. / Breccia, P. / Stott, A.J. / Aziz, O. / Birch, H.L. / Burli, R.W. / Hughes, S.J. / Jarvis, R.E. / Lamers, M. / Leonard, P.M. / Matthews, K.L. / Mcallister, G. / Pollack, S. ... Authors : Luckhurst, C.A. / Breccia, P. / Stott, A.J. / Aziz, O. / Birch, H.L. / Burli, R.W. / Hughes, S.J. / Jarvis, R.E. / Lamers, M. / Leonard, P.M. / Matthews, K.L. / Mcallister, G. / Pollack, S. / Saville-Stones, E. / Wishart, G. / Yates, D. / Dominguez, C. History Deposition May 22, 2015 Deposition site : PDBE / Processing site : PDBERevision 1.0 Feb 10, 2016 Provider : repository / Type : Initial releaseRevision 1.1 Jan 10, 2024 Group : Data collection / Database references ... Data collection / Database references / Derived calculations / Other / Refinement description Category : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_database_status / pdbx_initial_refinement_model / 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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