Entry Database : PDB / ID : 6fyz Structure visualization Downloads & linksTitle Development and characterization of a CNS-penetrant benzhydryl hydroxamic acid class IIa histone deacetylase inhibitor ComponentsHistone deacetylase 4 Details Keywords HYDROLASE / Hydroxamic acid / CNS-penetrant / HDAC4 inhibition / Class IIa HDAC inhibitorFunction / 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 : 2.15 Å DetailsAuthors Luckhurst, C.A. / Maillard, M.C. / Dominguez, C. CitationJournal : Bioorg. Med. Chem. Lett. / Year : 2019Title : Development and characterization of a CNS-penetrant benzhydryl hydroxamic acid class IIa histone deacetylase inhibitor.Authors: Luckhurst, C.A. / Aziz, O. / Beaumont, V. / Burli, R.W. / Breccia, P. / Maillard, M.C. / Haughan, A.F. / Lamers, M. / Leonard, P. / Matthews, K.L. / Raphy, G. / Stott, A.J. / Munoz-Sanjuan, ... Authors : Luckhurst, C.A. / Aziz, O. / Beaumont, V. / Burli, R.W. / Breccia, P. / Maillard, M.C. / Haughan, A.F. / Lamers, M. / Leonard, P. / Matthews, K.L. / Raphy, G. / Stott, A.J. / Munoz-Sanjuan, I. / Thomas, B. / Wall, M. / Wishart, G. / Yates, D. / Dominguez, C. History Deposition Mar 13, 2018 Deposition site : PDBE / Processing site : PDBERevision 1.0 Dec 5, 2018 Provider : repository / Type : Initial releaseRevision 1.1 Dec 26, 2018 Group : Data collection / Database references / Category : citationItem : _citation.journal_volume / _citation.page_first ... _citation.journal_volume / _citation.page_first / _citation.page_last / _citation.year Revision 1.2 Jan 17, 2024 Group : Data collection / Database references ... Data collection / Database references / Derived calculations / Refinement description Category : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_initial_refinement_model / pdbx_struct_conn_angle / struct_conn Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession ... _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_struct_conn_angle.ptnr1_auth_seq_id / _pdbx_struct_conn_angle.ptnr3_auth_seq_id / _pdbx_struct_conn_angle.value / _struct_conn.pdbx_dist_value / _struct_conn.ptnr1_auth_asym_id / _struct_conn.ptnr1_auth_comp_id / _struct_conn.ptnr1_auth_seq_id / _struct_conn.ptnr1_label_asym_id / _struct_conn.ptnr1_label_atom_id / _struct_conn.ptnr1_label_comp_id / _struct_conn.ptnr1_label_seq_id / _struct_conn.ptnr2_auth_asym_id / _struct_conn.ptnr2_auth_comp_id / _struct_conn.ptnr2_auth_seq_id / _struct_conn.ptnr2_label_asym_id / _struct_conn.ptnr2_label_atom_id / _struct_conn.ptnr2_label_comp_id
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