Nuclear Receptor Plasmids

Nuclear receptors (NRs) are a class of transcription factors that regulate gene transcription in response to ligand-binding. Ligands that bind to nuclear receptors include endogenous lipophilic small molecules such as steroid hormones, thyroid hormones, lipids, fatty acids, and retinoic acids. The modular structure of nuclear receptors contains the following domains: (A-B) N-terminal regulatory domain, (C) DNA-binding domain (DBD), (D) Hinge region, (E) Ligand binding domain (LBD), and (F) C-terminal domain. The regulation of gene expression by nuclear receptors usually happens when a ligand binding to a nuclear receptor which results in a conformational change in the receptor, receptor activation and subsequentially activation or repression of target genes.

In humans, the nuclear receptor superfamily comprises 48 members. The expression of a large number of genes is regulated by nuclear receptors, and many of these genes are involved in physiological processes (development, homeostasis, and metabolism) and play important roles in humans. Therefore, nuclear receptors are a major target class for therapeutic intervention to treat human diseases. To-date, a list of drugs targeting nuclear receptors have been approved.

RGBiotech offers a list of nuclear receptor plasmids that can be used in cell-based NR assays for screening agonists and antagonists of nuclear receptors. These plasmids contain the ligand-binding domain (LBD) of a specific nuclear receptor fused to the DNA-binding domain of GAL4. In combination with a reporter plasmid containing a luciferase reporter gene under the control of GAL4 binding sites, stable cell lines can be generated for in vitro cell assays. When a specific ligand binds to the LBD domain of the fusion protein, the fusion protein binds to the GAL4 binding sites, resulting in expression or repression of luciferase reporter gene.

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