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  • genes
  • These nuclear receptors are putative cancer therapy targets because they function as transcription factors that control the expression of many genes related to cell differentiation ( 1 , 2 ). (aacrjournals.org)
  • Ligand binding to nuclear receptors causes conformational changes in the receptor, resulting in a cascade of events, including dissociation of repressor proteins, association of coactivator proteins, and assembly of pol II and other transcriptional factors for activation of target genes. (thermofisher.com)
  • The RARs and RXRs bind to specific RA-responsive elements and regulate transcription of target genes in a ligand-dependent manner ( 5 - 6 ). (pnas.org)
  • Synthetic LXR agonist GW3965 improves glucose tolerance in a murine model of diet-induced obesity and insulin resistance by regulating genes involved in glucose metabolism in liver and adipose tissue. (wikipedia.org)
  • These hormone receptors sense a variety of metabolic ligands including lipophilic hormones, dietary fatty acids and their metabolites, and, depending on the varying levels of these ligands, control transcription of genes involved in balancing the changes in lipid balance in the body. (wikipedia.org)
  • In response, these receptors work with other proteins to regulate the expression of specific genes, thereby controlling the development, homeostasis, and metabolism of the organism. (wikipedia.org)
  • Nuclear receptors have the ability to directly bind to DNA and regulate the expression of adjacent genes, hence these receptors are classified as transcription factors. (wikipedia.org)
  • Because the expression of a large number of genes is regulated by nuclear receptors, ligands that activate these receptors can have profound effects on the organism. (wikipedia.org)
  • Many of these regulated genes are associated with various diseases, which explains why the molecular targets of approximately 13% of U.S. Food and Drug Administration (FDA) approved drugs target nuclear receptors. (wikipedia.org)
  • Here, CAR forms a heterodimer with retinoid X receptor (RXR) and interacts with the phenobarbital-responsive enhancer module (PBREM), a distal enhancer activating transcription of CAR target genes. (wikipedia.org)
  • steroid
  • Recent progress in the molecular and cellular biology of the nuclear steroid receptor superfamily has identified certain members as molecular targets for cancer therapy ( 1 ). (aacrjournals.org)
  • In this report, a mutant hMR, in which the residue Ala-773 facing the C11 steroid position was replaced by a glycine (A773G), was assayed for its capacity to bind steroids, to interact with receptor coactivators, and to stimulate transcription. (aspetjournals.org)
  • Ligands binding to CAR include bilirubin, a variety of foreign compounds, steroid hormones, and prescription drugs. (wikipedia.org)
  • In the absence of PB, the epidermal growth factor (EGF) binds to EGFR, thereby activating the steroid receptor coactivator-1 (Src1), which in turn phosphorylates RACK1. (wikipedia.org)
  • protein
  • LXRs regulate fatty acid synthesis by modulating the expression of sterol regulatory element binding protein-1c (SREBP-1c). (wikipedia.org)
  • Studies suggest that the protein represses nuclear hormone receptor-mediated transactivation via two separate steps: competition with coactivators and the direct effects of its transcriptional repressor function. (wikipedia.org)
  • The protein structure of RORα consists of four canonical functional groups: an N-terminal (A/B) domain, a DNA-binding domain containing two zinc fingers, a hinge domain, and a C-terminal ligand-binding domain. (wikipedia.org)
  • Ligand binding results in translocation of CAR from the cytosol into the nucleus, where the protein can bind to specific DNA sites, called response elements. (wikipedia.org)
  • When aggrecan monomers bind to hyaluronan in the presence of HAPLN1 (hyaluronanic acid and proteoglycan link protein 1), large, highly negatively charged aggregates form. (wikipedia.org)
  • antagonists
  • Assays developed using these reagents enable primary or secondary screening of nuclear receptor agonists and/or antagonists. (thermofisher.com)
  • TR-FRET based assays can be developed using the LanthaScreen® panel of fluorescein-labeled coregulator peptides to investigate conformational changes of nuclear receptors upon ligand binding, either by determining the affinity of ligand-bound receptor for different coregulator peptides, or by identifying additional agonists or antagonists via displacement or recruitment of a specific coregulator peptide. (thermofisher.com)
  • As antagonism of the RORγ receptor may have therapeutic applications in the treatment of inflammatory diseases, a number of synthetic RORγ receptor antagonists have been developed. (wikipedia.org)
  • potent
  • In contrast, C11-substituted steroids with a 17γ-lactonic ring displayed antagonist properties with hMR and acted as potent agonists with A773G. (aspetjournals.org)
  • Potent and specific RORγt inverse agonists are sought for treating TH17-related diseases such as psoriasis, rheumatoid arthritis, and type 1 diabetes. (nrresource.org)
  • Some of the most potent competitive reversible tyrosinase inhibitors are synthetic compounds with a potency hundreds of times that of kojic acid. (wikipedia.org)