Entry Database : PDB / ID : 8a9g Structure visualization Downloads & linksTitle Binary complex of 14-3-3 zeta Glucocorticoid Receptor (GR) pT524 peptide stabilised by (R)-para chloropyrrolidone1 Components14-3-3 protein zeta/delta Glucocorticoid receptor DetailsKeywords PROTEIN BINDING / 14-3-3 protein zeta/delta / Glucocorticoid Receptor / (R)-para chloropyrrolidone1 / protein-peptide complex / protein-protein interaction / PPI stabilisation / molecular glue / pyrrolidone1 analogueFunction / homology Function and homology informationFunction Domain/homology Component
Regulation of NPAS4 gene transcription / Golgi reassembly / regulation of glucocorticoid biosynthetic process / nuclear glucocorticoid receptor activity / regulation of synapse maturation / steroid hormone binding / NOTCH4 Activation and Transmission of Signal to the Nucleus / PTK6 Expression / neuroinflammatory response / glucocorticoid metabolic process ... Regulation of NPAS4 gene transcription / Golgi reassembly / regulation of glucocorticoid biosynthetic process / nuclear glucocorticoid receptor activity / regulation of synapse maturation / steroid hormone binding / NOTCH4 Activation and Transmission of Signal to the Nucleus / PTK6 Expression / neuroinflammatory response / glucocorticoid metabolic process / establishment of Golgi localization / microglia differentiation / maternal behavior / mammary gland duct morphogenesis / nucleus localization / Rap1 signalling / astrocyte differentiation / cellular response to glucocorticoid stimulus / negative regulation of protein localization to nucleus / motor behavior / KSRP (KHSRP) binds and destabilizes mRNA / regulation of gluconeogenesis / adrenal gland development / cellular response to steroid hormone stimulus / GP1b-IX-V activation signalling / Regulation of localization of FOXO transcription factors / Interleukin-3, Interleukin-5 and GM-CSF signaling / phosphoserine residue binding / Activation of BAD and translocation to mitochondria / estrogen response element binding / FOXO-mediated transcription of oxidative stress, metabolic and neuronal genes / SARS-CoV-2 targets host intracellular signalling and regulatory pathways / cellular response to glucose starvation / Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex / intracellular steroid hormone receptor signaling pathway / core promoter sequence-specific DNA binding / SARS-CoV-1 targets host intracellular signalling and regulatory pathways / RHO GTPases activate PKNs / negative regulation of TORC1 signaling / cellular response to transforming growth factor beta stimulus / HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand / TBP-class protein binding / steroid binding / negative regulation of innate immune response / cellular response to dexamethasone stimulus / regulation of ERK1 and ERK2 cascade / protein sequestering activity / synaptic transmission, glutamatergic / chromosome segregation / Translocation of SLC2A4 (GLUT4) to the plasma membrane / Deactivation of the beta-catenin transactivating complex / TP53 Regulates Metabolic Genes / RNA polymerase II transcription regulatory region sequence-specific DNA binding / Negative regulation of NOTCH4 signaling / Hsp90 protein binding / SUMOylation of intracellular receptors / spindle / DNA-binding transcription repressor activity, RNA polymerase II-specific / positive regulation of miRNA transcription / Nuclear Receptor transcription pathway / positive regulation of neuron apoptotic process / Regulation of RUNX2 expression and activity / nuclear receptor activity / melanosome / Circadian Clock / sequence-specific double-stranded DNA binding / gene expression / chromatin organization / DNA-binding transcription activator activity, RNA polymerase II-specific / blood microparticle / DNA-binding transcription factor binding / vesicle / Potential therapeutics for SARS / transmembrane transporter binding / DNA-binding transcription factor activity, RNA polymerase II-specific / mitochondrial matrix / nuclear speck / cadherin binding / RNA polymerase II cis-regulatory region sequence-specific DNA binding / DNA-binding transcription factor activity / cell division / protein phosphorylation / focal adhesion / negative regulation of DNA-templated transcription / centrosome / synapse / glutamatergic synapse / apoptotic process / ubiquitin protein ligase binding / chromatin / regulation of DNA-templated transcription / regulation of transcription by RNA polymerase II / negative regulation of apoptotic process / protein kinase binding / negative regulation of transcription by RNA polymerase II / signal transduction / positive regulation of transcription by RNA polymerase II / protein-containing complex / extracellular space / RNA binding Similarity search - Function Glucocorticoid receptor / Glucocorticoid receptor / 14-3-3 proteins signature 2. / 14-3-3 protein, conserved site / 14-3-3 proteins signature 1. / 14-3-3 protein / 14-3-3 homologues / 14-3-3 domain / 14-3-3 domain superfamily / 14-3-3 protein ... Glucocorticoid receptor / Glucocorticoid receptor / 14-3-3 proteins signature 2. / 14-3-3 protein, conserved site / 14-3-3 proteins signature 1. / 14-3-3 protein / 14-3-3 homologues / 14-3-3 domain / 14-3-3 domain superfamily / 14-3-3 protein / Nuclear hormone receptor / Nuclear hormones receptors DNA-binding region signature. / Zinc finger, nuclear hormone receptor-type / Zinc finger, C4 type (two domains) / Nuclear hormone receptors DNA-binding domain profile. / c4 zinc finger in nuclear hormone receptors / Nuclear hormone receptor, ligand-binding domain / Nuclear hormone receptor-like domain superfamily / Ligand-binding domain of nuclear hormone receptor / Nuclear receptor (NR) ligand-binding (LBD) domain profile. / Ligand binding domain of hormone receptors / Zinc finger, NHR/GATA-type Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 1.961 Å DetailsAuthors Munier, C.C. / Edman, K. / Perry, M.W.D. / Ottmann, C. Funding support European Union, 1items Details Hide detailsOrganization Grant number Country European Commission 675179 European Union
CitationJournal : J.Med.Chem. / Year : 2022Title : Designing Selective Drug-like Molecular Glues for the Glucocorticoid Receptor/14-3-3 Protein-Protein Interaction.Authors : Pallesen, J.S. / Munier, C.C. / Bosica, F. / Andrei, S.A. / Edman, K. / Gunnarsson, A. / La Sala, G. / Putra, O.D. / Srdanovic, S. / Wilson, A.J. / Wissler, L. / Ottmann, C. / Perry, M.W.D. / O'Mahony, G. History Deposition Jun 28, 2022 Deposition site : PDBE / Processing site : PDBERevision 1.0 Dec 28, 2022 Provider : repository / Type : Initial releaseRevision 1.1 Jan 4, 2023 Group : Database references / Category : citation / citation_authorItem : _citation.journal_volume / _citation.page_first ... _citation.journal_volume / _citation.page_first / _citation.page_last / _citation_author.identifier_ORCID Revision 1.2 Jan 31, 2024 Group : Data collection / Refinement descriptionCategory : chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_model
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