• In contrast, no ligands for the retinoic acid receptor-related orphan receptors beta and gamma (ROR beta and gamma) have been identified, yet structural data and structure-function analyses indicate that ROR beta is a ligand-regulated nuclear receptor. (nih.gov)
  • Subtypes include: Retinoic acid receptors (RARs) Retinoid X receptors (RXRs) RAR-related orphan receptors (RORs) Dyall SC, Michael GJ, Michael-Titus AT (2010). (wikipedia.org)
  • Our goal is to decipher the highly diverse functions of vitamin A, its active derivatives (retinoic acids), and the corresponding nuclear receptors (RARs/RXRs), in neural development, aging, and in stem cell control. (igbmc.fr)
  • 2005). The Retinoid X Receptors (RXRs) family (RXR alpha, beta, and gamma), preferentially bind 9-cis -RA and regulate gene transcription by forming heterodimers with a second family of RA receptors. (thermofisher.com)
  • Retinoids regulate gene expression through binding to the nuclear retinoic acid receptors (RARs) and retinoid X receptors (RXRs). (nih.gov)
  • With the identification of the family of nuclear retinoic acid receptors (RARs) and the discoveries of their effects on gene expression, the mechanism of retinoid action at the molecular level can now be investigated. (grantome.com)
  • Correlations of the results of retinoid transcriptional activation of and binding affinity for specific RARs with retinoid structure and the ability to regulate cell differentiation in more complex systems are invaluable for the efficient design of retinoids having enhanced chemopreventive effectiveness. (grantome.com)
  • Nuclear all-trans retinoic acid receptors (RARs) initiate early transcriptional events which engage pluripotent cells to differentiate into specific lineages. (pasteur.fr)
  • The responsiveness of genes to steroid hormones is principally mediated by functional interactions between DNA-bound hormone receptors and components of the transcriptional initiation machinery, including TATA-binding protein, TFIIB, or other RNA polymerase II associated factors. (umassmed.edu)
  • One postulated regulatory mechanism involves the functional antagonism between hormone receptors and nonreceptor transcription factors interacting at the same hormone response element. (umassmed.edu)
  • Peroxisome proliferator activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors that are related to retinoid, steroid and thyroid hormone receptors. (sigmaaldrich.com)
  • The nuclear hormone receptors liver X receptor α (LXRα) and LXRβ function as physiological receptors for oxidized cholesterol metabolites (oxysterols) and regulate several aspects of cholesterol and lipid metabolism. (aspetjournals.org)
  • These nuclear hormone receptors impact on hepatic triglyceride accumulation and insulin resistance. (wjgnet.com)
  • Molecular Biology of Peroxisome Proliferator Activated Receptors in Relation to Sebaceous Glands and Acne. (routledge.com)
  • Retinoid receptors are nuclear receptors (a class of proteins) that bind to retinoids. (wikipedia.org)
  • Like other TNF-family receptors and the IL-1 receptor, RANK mediates its signal transduction via TNF receptor-associated factor (TRAF) proteins, suggesting that the signaling pathways activated by RANK and other inflammatory cytokines involved in osteoclast differentiation and activation are interconnected. (umassmed.edu)
  • A greater understanding of the mechanism of transcriptional regulation by nuclear receptors has lead to the identification of multiple accessory proteins that bind to the nuclear receptors in a ligand-dependent manner. (sigmaaldrich.com)
  • The nuclear receptor corepressor (N-CoR) or silencing mediator of retinoid and thyroid receptors (SMRT) proteins bind and mediate repression of transcription by the unliganded receptors. (sigmaaldrich.com)
  • 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)
  • Regulation of gene transcription is controlled in part by nuclear receptors that function coordinately with coregulator proteins. (aspetjournals.org)
  • The drug mediates interactions between these receptors, growth factors, and proteins within that pathway to reduce new abnormal bone formation. (medscape.com)
  • CD3254 a selective agonist of retinoid -X- receptor (RXR). (targetmol.com)
  • AGN-191659 is a Retinoid X Receptor (RXR) pan-agonist. (targetmol.com)
  • Izumerogant is an inverse agonist of the retinoid -related orphan receptor -gamma (RORγ). (targetmol.com)
  • GW0791 is a retinoid X receptor α (RXRα) agonist. (targetmol.com)
  • AGN 191701 is an agonist of the Retinoid X receptor . (targetmol.com)
  • TBTC is a selective agonist of retinoid X receptor α that acts by improving behavioral deficit in Alzheimer's disease mo. (targetmol.com)
  • ROR Modulator I is the first potent inverse agonist of the retinoid -related orphan receptor . (targetmol.com)
  • Bexarotene (Bxt) is a retinoid-X receptor agonist used in the treatment of cutaneous lymphoma with a favorable safety profile whose effects have been recently investigated in other neurodegenerative diseases. (frontiersin.org)
  • As an agonist of the retinoic-X receptor (RXR) pathway, Bxt notably increased the nuclear expression of the RXRα throughout transcriptionally active euchromatin domains. (frontiersin.org)
  • We propose to develop receptor- specific retinoids and antagonists for chemoprevention of cancers induced in epithelial tissues. (grantome.com)
  • We also investigate the therapeutic potential of specific retinoids in neurological and psychiatric diseases. (igbmc.fr)
  • When bound to a retinoid, they act as transcription factors, altering the expression of genes with corresponding response elements. (wikipedia.org)
  • Cotransfection assays showed that RXR, but not RAR, activates apo C-III transcription through this element either as a homo- or as a heterodimer with the peroxisome proliferator-activated receptor. (tno.nl)
  • Nuclear receptors (NRs) are conditional transcription factors with common multidomain organization that bind diverse DNA elements. (houstonmethodist.org)
  • Leptin and adiponectin can augment the oxidation of fatty acid in liver by activating the nuclear receptor super-family of transcription factors, namely peroxisome proliferator-activated receptor (PPAR)-α. (wjgnet.com)
  • Furthermore, results obtained from mammalian two-hybrid experiments assessing various domain configurations of the respective receptors showed that full-length DAX-1 inhibited the CAR-SRC1 interaction by approximately 50%, whereas the same interaction was restored to 90% of control when the DAX-1 transcription silencing domain was deleted. (aspetjournals.org)
  • Here we report the crystal structure of the human retinoid X receptor α-liver X receptor β (RXRα-LXRβ) heterodimer on its cognate element, an AGGTCA direct repeat spaced by 4 nt. (houstonmethodist.org)
  • ATRA and related retinoids inhibit ROR beta but not ROR alpha transcriptional activity suggesting that high-affinity, subtype-specific ligands could be designed for the identification of ROR beta target genes. (nih.gov)
  • We show that YY1 and vitamin D receptor (VDR)/retinoid X receptor heterodimers compete for binding at the osteocalcin VDRE. (umassmed.edu)
  • PPAR-RXR heterodimers can also be activated by ligand binding to either receptor partner independently. (sigmaaldrich.com)
  • The peroxisome proliferator-activated receptor γ (PPARγ) is highly expressed in the colon mucosa and its activation has been reported to protect against colitis. (hal.science)
  • We studied the involvement of PPARγ and its heterodimeric partner, the retinoid X receptor (RXR) in intestinal inflammatory responses. (hal.science)
  • The recognition of microbial pathogens by the innate immune system involves Toll-like receptors (TLRs), which recognize pathogen-associated molecular patterns. (umassmed.edu)
  • Using nondenaturing mass spectrometry and scintillation proximity assays we found that all-trans retinoic acid (ATRA) and several retinoids bind to the ROR beta ligand-binding domain (LBD). (nih.gov)
  • However, random variations (noise) that affect how many of these molecules are produced, how they move through the space between cells and how they bind to receptors makes the reality much more complex. (elifesciences.org)
  • However, systemic toxicity and teratogenicity have hindered the development of natural and synthetic retinoids as useful drugs for the chemoprevention of cancer. (grantome.com)
  • Side effects were typical of those seen with other systemic retinoid drugs, including mucocutaneous events such as dryness of the skin and mucous membranes, alopecia, drug eruption , rash, and pruritus, and musculoskeletal events, such as arthralgia and premature growth plate closure in growing children. (medscape.com)
  • Because of the significant long-term adverse effects, reserve systemic retinoids for severe disease that is refractory to conventional therapy. (medscape.com)
  • Our results identify ROR beta as a retinoid-regulated nuclear receptor, providing a novel pathway for retinoid action. (nih.gov)
  • Taken orally, palovarotene selectively targets the gamma subtype of retinoic acid receptors that regulate skeletal development and ectopic bone in the retinoid signaling pathway. (medscape.com)
  • In this study, we analyzed whether retinoids increase the expression of apo C- III, an antagonist of plasma triglyceride catabolism. (tno.nl)
  • [ 11 ] Loss of 2 of the retinoid receptors (RXR-beta and RXR-gamma) seems apparent in sebaceous carcinoma. (medscape.com)
  • Significant age-related declines in the levels of retinoid receptors in the forebrains of rats have been reversed by supplementation with the omega-3 fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), which can restore neurogenesis. (wikipedia.org)
  • Thus RAR establishes physical and functional links with components of the elongation complex, enabling the rapid retinoid-induced induction of genes required for neuronal differentiation. (pasteur.fr)
  • Studies in osteoclast biology have led to the identification of factors responsible for the differentiation and activation of osteoclasts, the most important of which is the receptor activator of NF-kappa B ligand/osteoclast differentiation factor (RANKL/ODF), a tumor necrosis factor (TNF)-like protein. (umassmed.edu)
  • In this report, DAX-1, a nuclear receptor family member with corepressor properties, was identified as a potent CAR regulator. (aspetjournals.org)
  • There is experimental evidence suggesting that retinoids may be involved in ALS pathogenesis. (frontiersin.org)
  • Biochemical analyses have also identified some pathways potentially involved in ALS pathogenesis, including retinoid pathways. (frontiersin.org)
  • A growing body of literature implicates the peroxisome proliferators-activated receptors (PPARs) in the pathogenesis and treatment of NAFLD. (wjgnet.com)
  • In addition to promoter sequences, RAR binds to genomic, transcribed regions of retinoid-regulated genes, in association with RNA polymerase II and as a function of P-TEFb activity. (pasteur.fr)
  • Each receptor shows a differential pattern of tissue expression and is activated by structurally diverse compounds including endogenous long-chain fatty acids. (sigmaaldrich.com)
  • Clusters of retinoid-regulated genes were selectively dependent on BRD4 and/or AF9 expression, which correlated with RAR association to transcribed regions. (pasteur.fr)
  • Recombinant full length protein corresponding to Human Retinoid X Receptor beta/RXRB. (abcam.com)
  • In human hepatoma HepG2 cells, retinoids increased apo C-III mRNA and protein production. (tno.nl)
  • PPARs have a highly conserved DNA binding domain (region C) and a diverse ligand-independent activation domain (region A/B) which can confer constitutive activity on the receptor. (sigmaaldrich.com)
  • The correlations between hydroxytryptamine receptor 2A (HTR2A) gene polymorphisms (1438A/G, 102T/C, and rs7997012G/A) and the safety and efficacy of antidepressants in depression patients have been reported. (cdc.gov)
  • Hypertriglyceridemia is a metabolic complication of retinoid therapy. (tno.nl)
  • Mutagenesis experiments localized the retinoid responsiveness to a cis- element consisting of two imperfect AGGTCA sequences spaced by one oligonucleotide (DR-1), within the previously identified C3P footprint site. (tno.nl)
  • Hence, the vitamin D receptor (VDR) is highly expressed in kidney tissue [ 3-5 ]. (karger.com)
  • Retinoids prevent and reverse the process of neoplastic transformation and inhibit tumor promotion. (grantome.com)
  • To do so, cells release signaling molecules that can move around within a tissue and be detected by receptors on other cells. (elifesciences.org)
  • Toll-like diseases and causes severe and long-lasting health problems in the case of chronifi- receptor. (cdc.gov)