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Nuclear Receptor Coactivator 2Nuclear Receptor Coactivator 1Nuclear Receptor CoactivatorsHistone AcetyltransferasesNuclear Receptor Coactivator 3CREB-Binding ProteinTranscription Factorsp300-CBP Transcription FactorsTrans-ActivatorsE1A-Associated p300 ProteinTranscriptional ActivationNuclear ProteinsMediator Complex Subunit 1AcetyltransferasesTranscription, GeneticReceptors, Cytoplasmic and NuclearProtein BindingProtein-Arginine N-MethyltransferasesNuclear Receptor Co-Repressor 1Promoter Regions, GeneticEstrogen Receptor alphaProtein Structure, TertiaryDNA-Binding ProteinsReceptors, Thyroid HormoneReceptors, AndrogenGene Expression RegulationCOS CellsAcetylationReceptors, Retinoic AcidTwo-Hybrid System TechniquesReceptors, EstrogenLigandsRepressor ProteinsAdenovirus E1A ProteinsBinding SitesCell LineReceptors, SteroidTransfectionNuclear Receptor Co-Repressor 2Receptors, CalcitriolRecombinant Fusion ProteinsMolecular Sequence DataHeLa CellsResponse ElementsAmino Acid SequenceChromatinHistonesRetinoid X ReceptorsAmino Acid MotifsMediator ComplexGlutathione TransferaseHerpes Simplex Virus Protein Vmw65Genes, ReporterCyclic AMP Response Element-Binding ProteinEstrogen Receptor betaCell NucleusReceptors, GlucocorticoidNuclear Respiratory FactorsSaccharomyces cerevisiae ProteinsLuciferasesSelective Estrogen Receptor ModulatorsSignal TransductionCell Line, TumorCo-Repressor ProteinsPrecipitin TestsNF-E2-Related Factor 1Hepatocyte Nuclear Factor 4Transcription Factor TFIIDReceptors, ProgesteroneDimerizationCarrier ProteinsTATA-Box Binding ProteinModels, BiologicalHistone DeacetylasesCell Cycle ProteinsMutationChromatin ImmunoprecipitationThyroid Hormone Receptors betaCercopithecus aethiopsCdh1 ProteinsEstrogen Receptor ModulatorsPlasmidsBase SequenceBALB 3T3 CellsRNA, MessengerEstrogensAndrogensReceptor Cross-TalkReverse Transcriptase Polymerase Chain ReactionTamoxifenOncogene ProteinsF-Box MotifsSequence Homology, Amino AcidGene Products, taxEnhancer Elements, GeneticChromatin Assembly and DisassemblyNuclear Respiratory Factor 1SuntanTumor Cells, CulturedRNA Polymerase II
SteroidRecruitment of coactivatorsP300PeroxisomeProteinsCorepressorsProteinChromatinReceptorsVariantsNCOA3BindsSRC3CanonicalTRAP220MotifsGeneMediatorActsFunctionsFoundSteroid receptorDefined as a transcriptional coactivatorTranscriptional coactivatorsCREBPeptideComplexesArginine methyltransferasePeroxisomeHistonePolymeraseSAGAComplexRolesInteractionYeastGeneCellularInteractionsEP300BindGeneticInhibitsActivityFunctionHumanDomain
Steroid9
  • Here, we determined that upregulation of the oncogenic transcriptional coregulator steroid receptor coactivator 2 (SRC-2), also known as NCOA2, drives glutamine-dependent de novo lipogenesis, which supports tumor cell survival and eventual metastasis. (jci.org)
  • Through biochemical and crystallographic studies, we identify that steroid receptor coactivator-3 (SRC3) (also named as amplified in breast cancer-1 or AIB1) interacts strongly with AR via synergistic binding of its first and third LXXLL motifs. (rcsb.org)
  • Cyclin-dependent kinase 2 (Cdk2)/cyclin A is a novel PR coregulator that binds the NTD and acts by phosphorylating steroid receptor coactivator-1 and modulating steroid receptor coactivator-1 interaction with PR. (nih.gov)
  • Given the established role of estrogens in breast cancer, we hypothesized that coding variation in steroid receptor coactivator and corepressor genes may alter inter-individual response to estrogen and serve as markers of breast cancer risk. (biomedcentral.com)
  • Cellular response to estrogens is mediated through estrogen receptors (ERα and ERβ), which upon binding to ligand and DNA hormone response elements, recruit coactivator and corepressor proteins that regulate the expression of steroid hormone target genes. (biomedcentral.com)
  • In this study, we systematically screened the coding exons of steroid hormone receptor coactivator and corepressor genes in a multiethnic panel of women with breast cancer in an attempt to identify and catalogue potentially functional coding polymorphisms that may serve as genetic markers of breast cancer risk. (biomedcentral.com)
  • Our studies also demonstrate that Tip60 co-immunoprecipitates with the full-length AR in vitro and that, in our system, Tip60 enhances transactivation to levels observed with the coactivators steroid receptor coactivator 1, p300, and CREB-binding protein. (ox.ac.uk)
  • Obesity due to Steroid Receptor Coactivator-1 deficiency is associated with endocrine and metabolic abnormalities. (ox.ac.uk)
  • CONTEXT: Genetic variants affecting the nuclear hormone receptor coactivator Steroid Receptor Coactivator, SRC-1, have been identified in people with severe obesity and impair melanocortin signaling in cells and mice. (ox.ac.uk)
Recruitment of coactivators2
  • 11 ] The relative recruitment of coactivators versus corepressors for a given ligand (e.g. estradiol vs tamoxifen) is tissue specific and may account for agonist vs. antagonist activity of the same ligand in different tissues. (biomedcentral.com)
  • The binding of ligand triggers a series of events which result in conformational changes involving recruitment of coactivators and dissociation of corepressors. (sigmaaldrich.com)
P3004
  • The histone acetyltransferase (Head wear) p300/CBP is a transcriptional coactivator implicated in lots of gene regulatory pathways and protein acetylation events. (woofahs.com)
  • p300/CBP frequently acts as a transcriptional coactivator and continues to be recommended to bind to a variety of essential transcription elements (Goodman and Smolik, 2000). (woofahs.com)
  • The transcriptional coactivator p300/CBP (CREBBP) is a histone acetyltransferase (HAT) that regulates gene expression by acetylating histones and other transcription factors. (umassmed.edu)
  • Coactivator proteins such as SRC1 and CBP/p300 are recruited by agonist bound receptors and promote initiation of transcription by remodelling the chromatin structure while coactivators such as the PPAR binding protein (PBP) and TRAP220 interact directly with the transcriptional machinery. (sigmaaldrich.com)
Peroxisome5
  • Recent studies have identified the transcriptional coactivator peroxisome proliferator-activated receptor γ coactivator-1 (PGC-1) as a regulator of mitochondrial function in tissues specialized for thermogenesis, such as brown adipose. (jci.org)
  • Peroxisome proliferator-activated receptor γ coactivator-1α (PGC-1α) is capable of coactivating several nuclear receptors and transcription factors that participate in the regulation of multiple metabolic processes, including gluconeogenesis, mitochondrial biogenesis, and adaptive thermogenesis. (aspetjournals.org)
  • The transcriptional coactivator peroxisome proliferator activated receptor (PPAR)gamma coactivator-1 alpha and the nuclear receptor PPAR alpha control the expression of glycerol kinase and metabolism genes independently of PPAR gamma activation in human white adipocytes. (unil.ch)
  • We hypothesized that the PPARα coactivator peroxisome proliferator-activated receptor gamma coactivator-1 alpha (PGC-1α) is necessary for mitochondrial biogenesis in insulin resistant hearts and that this response was adaptive. (wustl.edu)
  • Peroxisome proliferator-activated receptor-binding protein (PBP), also known as thyroid hormone receptor-associated protein 220/vitamin D receptor-interacting protein 205/mediator 1, an anchor for multisubunit mediator transcription complex, functions as a transcription coactivator for nuclear receptors. (wustl.edu)
Proteins1
  • Alternatively nuclear receptor coactivators can function as adaptor proteins that bring nuclear receptors into close proximity with transcriptional complexes. (bvsalud.org)
Corepressors1
  • RAR-controlled transactivation depends mostly on agonist-induced structural transitions in RAR C-terminus (AF-2), thus bridging coactivators or corepressors to chromatin, hence controlling preinitiation complex assembly. (pasteur.fr)
Protein2
  • Indeed, mass spectrometry fingerprinting identified the Bromodomain-containing protein 4 (BRD4) and ALL1-fused gene from chromosome 9 (AF9/MLLT3), known to associate with and regulates the activity of Positive Transcription Elongation Factor b (P-TEFb), as novel RAR coactivators. (pasteur.fr)
  • In this report, we show that Tip60, which was originally identified as a coactivator for the human immunodeficiency virus TAT protein, can enhance AR-mediated transactivation in a ligand-dependent manner in LNCaP and COS-1 cell lines. (ox.ac.uk)
Chromatin1
  • The coactivators may act through an enzymatic process that affects the rate of transcription or the structure of chromatin. (bvsalud.org)
Receptors1
  • AR is distinguished from other nuclear receptors in that after hormone binding, it preferentially responds to a specialized set of coactivators bearing aromatic-rich motifs, while responding poorly to coactivators bearing the leucine-rich "NR box" motifs favored by other nuclear receptors. (escholarship.org)
Variants1
  • Cataloging and testing of coding variants in coactivator and corepressor genes should continue and may serve as a valuable resource for investigations of other hormone-related phenotypes, such as inter-individual response to hormonal therapies used for cancer treatment and prevention. (biomedcentral.com)
NCOA31
  • also known as NCOA3 or AIB1) is a member of the multifunctional p160/SRC family of coactivators, which also includes SRC-1 and SRC-2. (frontiersin.org)
Binds2
SRC31
  • Mutagenesis and functional studies confirm that SRC3 is a preferred coactivator for hormone-activated AR. (rcsb.org)
Canonical3
  • This is because AR, unlike any other nuclear receptor, prefers its own N-terminal FXXLF motif to the canonical LXXLL motifs of coactivators. (rcsb.org)
  • However, during prostate cancer, abnormal association with such coactivators, as well as with coactivators containing canonical leucine-rich motifs, promotes disease progression. (escholarship.org)
  • Structures of AR in complex with FxxLF, LxxLL, FxxLW, WxxLF, WxxVW, FxxFF, and FxxYF motifs reveal a changing surface of the AR coactivator binding interface that permits accommodation of both AR-specific aromatic-rich motifs and canonical leucine-rich motifs. (escholarship.org)
TRAP2201
  • We conclude that transcription coactivator PBP/TRAP220/MED1 is involved in the regulation of hepatic CAR function and that PBP deficiency in liver abrogates acetaminophen hepatotoxicity. (wustl.edu)
Motifs2
  • Under normal conditions, interactions with these AR-specific coactivators through aromatic-rich motifs underlie targeted gene transcription. (escholarship.org)
  • Induced fit provides perfect mating of the motifs representing the known family of AR coactivators and suggests a framework for the design of AR coactivator antagonists. (escholarship.org)
Gene1
  • Although the underlying mechanisms are less clear, gene regulatory abilities of coactivators can bridge the transcription functions of AR and NF-κB. (mssm.edu)
Mediator1
  • Mediator is a multiprotein complex that functions as a transcriptional coactivator in all eukaryotes. (wikipedia.org)
Acts1
  • RBPJ can function as a coactivator when Notch signaling is activated but acts as a repressor in the absence of a Notch stimulus. (mdpi.com)
Functions1
  • Although the full-length PBP only minimally increased CAR transcriptional activity, a truncated form of PBP (amino acids 487-735) functioned as a dominant negative repressor, establishing that PBP functions as a coactivator for CAR. (wustl.edu)
Found1
  • [ 4 ] a similar transcriptional coactivator located on chromosome 22q13, have also been found in patients with a Rubinstein-Taybi syndrome (RSTS) phenotype. (medscape.com)
Steroid receptor6
  • In the keratinocyte the major coactivator complexes include the vitamin D interacting protein (DRIP) complex and the steroid receptor coactivator (SRC) complexes. (nih.gov)
  • Through biochemical and crystallographic studies, we identify that steroid receptor coactivator-3 (SRC3) (also named as amplified in breast cancer-1 or AIB1) interacts strongly with AR via synergistic binding of its first and third LXXLL motifs. (rcsb.org)
  • The recently identified steroid receptor coactivator (SRC) family contains three homologous members that can enhance transcriptional activities of NRs and certain non-NR transcription factors. (jneurosci.org)
  • Members of the steroid receptor coactivator (SRC) family, which include SRC-1 (NcoA-1/p160), SRC-2(TIF2/GRIP1/NcoA-2) and SRC-3(pCIP/RAC3/ACTR/pCIP/ AIB1/TRAM1), are critical mediators of steroid receptor action. (nih.gov)
  • A more precise identification of the molecular pathways regulated by these coactivators is crucial for understanding the role of steroid receptor coactivators in the control of energy homeostasis and obesity. (nih.gov)
  • Many cofactors, such as corepressors (nuclear receptor corepressor, silencing mediator of retinoid and thyroid hormone receptors, etc.) and coactivators (steroid receptor coactivator-1 and cyclic AMP response element binding-binding protein, etc.), are also involved in the regulation of targeted genes. (medscape.com)
Defined as a transcriptional coactivator1
  • CBP was initially defined as a transcriptional coactivator that, as a result of its large size and multiple protein binding domain modules, may function as a molecular scaffold. (nih.gov)
Transcriptional coactivators1
  • Although cAMP response element-binding protein (CREB) and its coactivators-the cAMP-regulated transcriptional coactivators (CRTCs)-mediate transcriptional effects of cAMP in most tissues, other transcription factors such as ATF2 appear critical for induction of thermogenic genes by cAMP in BAT. (nih.gov)
CREB2
  • Here, we identify acetyl-lysine competitive inhibitors targeting the bromodomains of coactivators CREB (cyclic-AMP response element binding protein) binding protein (CBP) and E1A binding protein of 300 kDa (EP300) as potent enhancers of reprogramming. (ox.ac.uk)
  • Since nerve growth factor (NGF) receptor and brain-derived neurotrophic factor receptor signaling through CREB requires p300 and PCAF histone acetyltransferases, we sought to determine whether HIV-1 Tat coactivator interactions interfere with neurotrophin receptor signaling in neuronal cells. (elsevierpure.com)
Peptide1
  • Although ( R )-all- trans -13,14-dihydroretinoic acid exhibited comparable potency to retinoic acid in promoting the interaction of RARs with a coactivator peptide in vitro, its potency in activating RAR-controlled genes in cell-based assays was much lower than that of retinoic acid. (aspetjournals.org)
Complexes5
  • Abstract: DESCRIPTION (provided by applicant): The transcriptional activity of the vitamin D receptor (VDR) is regulated by a number of coactivator and corepressor complexes, which bind to the VDR in a ligand (1,25(OH)2D3) dependent (coactivators) or inhibited (corepressors) process. (nih.gov)
  • These coactivator complexes are not interchangeable in their regulation of keratinocyte proliferation and differentiation. (nih.gov)
  • Hypothesis: The two main coactivator complexes, DRIP and SRC, differentially modulate the ability of VDR, its ligand 1,25(OH)2D3 and their interactions with 2-catenin to inhibit keratinocyte proliferation, while promoting keratinocyte differentiation leading to a protective epidermal barrier and normal hair follicle cycling. (nih.gov)
  • We investigate the structure and function of the yeast transcriptional coactivator complexes TFIID and SAGA, which bind TBP and load it onto gene promoters in a highly controlled way. (igbmc.fr)
  • Gene transcription by RNA polymerase II is regulated by activator proteins that recruit the coactivator complexes SAGA (Spt-Ada-Gcn5- acetyltransferase )1,2 and transcription factor IID ( TFIID )2-4. (bvsalud.org)
Arginine methyltransferase1
  • Intriguingly, EA treatment was also associated with reduced histone 3 arginine 17 methylation levels (H3R17me2), implying the inhibitory role of EA in coactivator-associated arginine methyltransferase 1 (CARM)1 activity during adipogenesis. (unl.edu)
Peroxisome4
  • Here we describe a mechanism by which insulin, through the intermediary protein kinase Akt2/protein kinase B (PKB)-β, elicits the phosphorylation and inhibition of the transcriptional coactivator peroxisome proliferator-activated receptor-coactivator 1α (PGC-1α), a global regulator of hepatic metabolism during fasting. (nature.com)
  • Several known and putative coactivators were isolated, including glucocorticoid receptor-interacting protein-1 (GRIP-1) and peroxisome proliferator-activated receptor (PPAR)-binding protein (PBP/TRAP220/DRIP205). (pasteur.fr)
  • SMAD3 negatively regulates serum irisin and skeletal muscle FNDC5 and peroxisome proliferator-activated receptor γ coactivator 1-α (PGC-1α) during exercise. (nih.gov)
  • CusabioMouse Peroxisome proliferator-activated receptor gamma coactivator 1-alpha. (joplink.net)
Histone2
  • SAGA and NuA4 are prototypical examples of coactivators containing a Histone Acetyl Transferase activity coupled to other functions, specific to each complex. (igbmc.fr)
  • Defect of histone acetyltransferase activity of the nuclear transcriptional coactivator CBP in Rubinstein-Taybi syndrome. (nih.gov)
Polymerase1
  • These proteins, termed coactivators, often have intrinsic enzymatic activity or act to recruit other proteins with enzymatic activities that modify chromatin associated proteins, as well as AR, other coactivators and polymerase. (fiu.edu)
SAGA1
  • Structure of the transcription coactivator SAGA. (bvsalud.org)
Complex2
  • We found that the DRIP complex is the main complex binding to VDR in the proliferating keratinocyte, whereas SRC3 and its associated proteins is the major coactivator binding to VDR in the differentiated keratinocyte. (nih.gov)
  • The control of viral IE expression is complex with regulatory mechanisms involving multiple transcription factors, coactivators, elongation factors, and epigenetic machinery that converge to determine IE expression (Fig. 2). (nih.gov)
Roles4
  • Vertebrate coactivators play important roles in development, cell differentiation, STEM cell maintenance, apoptosis or aging, and are involved in several genetic diseases and cancer. (igbmc.fr)
  • This chapter summarizes the current evidence for the roles for these coactivators in prostate cancer based on their contributions to AR action, cell growth and their expression levels in prostate tumors. (fiu.edu)
  • The estrogen-related receptor alpha (ERRalpha) and proliferator-activated-receptor-gamma coactivator-1alpha (PGC-1alpha) play major roles in transcriptional control of cellular energy metabolism. (nih.gov)
  • A particular emphasis has been on the roles of the cellular transcriptional coactivator HCF-1 during the initiation of lytic infection and reactivation from latency. (nih.gov)
Interaction2
  • Many candidate coactivators have been identified through interaction and overexpression studies. (fiu.edu)
  • XCT790 inhibits ERRalpha activity by disrupt its interaction with coactivator and its stability. (nih.gov)
Yeast3
  • Environmental estrogens induce transcriptionally active estrogen receptor dimers in yeast: activity potentiated by the coactivator RIP140. (nih.gov)
  • Thus we have identified several potential RORalpha coactivators that, in contrast to the interactions with hormone receptors, interact with RORalpha in yeast, in bacterial extracts, and in mammalian cells in vivo and in vitro in the absence of exogenous ligand. (pasteur.fr)
  • GRIP-1 functioned as a coactivator for the RORalpha both in yeast and in mammalian cells. (pasteur.fr)
Gene1
  • 20. Coactivators in gene regulation by STAT5. (nih.gov)
Cellular1
  • Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming. (ox.ac.uk)
Interactions3
  • Furthermore, these observations indicate the potential for discovering small molecules that by selectively modulating the interactions between the coactivators and VDR can manifest specificity in regulating VDR function not achievable by ligands such as 1,25(OH)2D3 and its analogs. (nih.gov)
  • Here, we demonstrate that Tat-coactivator interactions inhibit NGF- and brain-derived neurotrophic factor-responsive CRE trans-activation and neurotrophin protection against apoptosis in PC12 and IMR-32 neuroblastoma cells. (elsevierpure.com)
  • Importantly, these findings suggest that HIV-1 Tat-coactivator interactions may contribute to neurotrophin signaling impairments and neuronal apoptosis associated with HIV-1 infections of the CNS. (elsevierpure.com)
EP3003
  • In contrast, catalytic inhibition of CBP/EP300 prevents iPSC formation, suggesting distinct functions for different coactivator domains in reprogramming. (ox.ac.uk)
  • To further elucidate the role of these two coactivators, we conditionally knocked out Ep300 and/or CrebBP in differentiating rods or cones, using opsin-driven Cre recombinase. (wustl.edu)
  • Interestingly, the presence of a single wild-type allele of either coactivator prevented many of these defects, with Ep300 more effective than Cbp. (wustl.edu)
Bind1
  • We provide a structural rationalization for D box and KEN box recognition by coactivators and demonstrate that many noncanonical APC/C degrons bind APC/C coactivators at the D box coreceptor. (rcsb.org)
Genetic1
  • 2013) now suggest that nuclear receptor coactivator 5 (NCOA5) provides a genetic link between the two diseases through its effects on hepatic IL-6 expression. (nih.gov)
Inhibits1
  • Ellagic acid inhibits adipocyte differentiation through coactivator-as" by Inhae Kang, Meshail Okla et al. (unl.edu)
Activity2
  • We have discovered that different coactivators, DRIP and SRC in particular, regulate the transcriptional activity of VDR differently for different genes, and thus selectively affect different functions in the keratinocyte. (nih.gov)
  • The ERR reporter cell line detects its endogenous ERR activity using the coactivator expressing in the 293T cells, while PGC/ERR reporter cell line measures the ERR activity in the presence of its specific coregulator, PGC. (nih.gov)
Function1
  • Sp110 localizes to the PML-Sp100 nuclear body and may function as a nuclear hormone receptor transcriptional coactivator. (medlineplus.gov)
Human2
  • To determine human PPARgamma coactivator-1 (PGC-1) amino acid sequence and to study PGC-1 mRNA tissue distribution. (nih.gov)
  • Human activating signal cointegrator 1 (hASC-1) was originally isolated as a transcriptional coactivator of nuclear receptors. (korea.ac.kr)
Domain1
  • We therefore searched for mammalian RORalpha coactivators using the minimal activation domain as bait in a two-hybrid screen. (pasteur.fr)