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> Nuclear Hormone Receptor & Regulator Nuclear Hormone Receptor & Regulator
Nuclear hormone receptors are ligand-dependent transcription factors that regulate gene expression in response to a wide range of developmental, physiological, and environmental cues. Signal transduction via NRs is unusual in that the hormone ligand forms an integral part of the protein complex involved in DNA binding and transcriptional activation. NRs are key targets for drug development as many are implicated in diabetes and other endocrine disorders as well as cancer.
Sino Biological offers a comprehensive set of tools for nuclear hormone receptor & regulator related studies, including recombinant proteins, antibodies (rabbit mAbs, mouse mAbs, rabbit pAbs), ELISA kits, and ORF cDNA clones.
Nuclear Hormone Receptor & Regulator Products
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Nuclear Receptor
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Nuclear Hormone Receptor Coregulators
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Nuclear Hormone Receptor & Regulator Background
Nuclear hormone receptors (NRs) are ligand-dependent transcription factors involved in growth, differentiation, development, and maintenance of cellular homeostasis. Signal transduction via NRs is unusual in that the hormone ligand forms an integral part of the protein complex involved in DNA binding and transcriptional activation. NRs share common functional domains named A to F. The N-terminal A/B region is weakly conserved. The conserved C domain is the DNA-binding domain, which consists of two zinc-finger-like motifs. The D domain is a variable hinge. The multifunctional C-terminal half of the protein (domain E) encompasses the ligand-binding domain (LBD), a second activation function (AF-2), a dimerization domain, and a region involved in nuclear localization. The AF-2 autonomous activation domain (AF-2 AD) is composed of an amphipathic α-helix that is highly conserved among nuclear receptors and is critical for transcriptional activation. The most C-terminal region (domain F) is variable and has no known function.
Nuclear hormone receptors can be divided into Type I and Type II receptors. Type I receptors comprise the classical steroid hormone receptors such as the receptors for estrogen, progestins, glucocorticoids, androgens, and minearalocorticoids. Type I receptors bind their cognate DNA sequences as homodimers and occasionally as monomers. Type II receptors include the thyroid hormone receptors, receptors for retinoids, lipids, 1,25-dihydroxy-vitamin D3, cholesterol metabolites, and xenobiotics. Type I receptors bind their cognate sequences as homodimers, while Type II receptors primarily bind to their target genes as heterodimers with the retinoid x receptors. The process of an inactive aporeceptor to a transcriptionally active form is complex: 1) binding with ligands such as endocrine hormones, fatty acids, cholesterol derivatives and products of lipid metabolism, 2)change in the conformation of the NR to an active form which allows for, 3) interaction with other co-regulator proteins which potentiate the ability of the NR to activate or repress transcription of target genes.
Coregulators have the faculty to repress (corepressors) or to enhance (coactivators) the activity of genes regulated by nuclear hormone receptors in a ligand-dependent fashion.
Nuclear Hormone Receptor & Regulator Related Studies
- Evans RM. (1988) The steroid and thyroid hormone receptor superfamily. Science. 240(4854):889-95.
- Olefsky JM. (2001) Nuclear receptor minireview series. J Biol Chem. 276(40):36863-4.
- Mangelsdorf DJ, et al. (1995) The nuclear receptor superfamily: the second decade. Cell. 83(6):835-9.
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