Nuclear hormone receptors (NHRs) are ligand-activated transcription factors that regulate diverse physiological and cellular events. Ligand binding to nuclear receptors (such as type I) result in its translocation from the cytoplasm into the cell nucleus and binding to nuclear hormone response elements. A large number of genes are regulated by nuclear receptors; many are known to be associated with various human diseases.

Nuclear hormone receptors are important targets for drug development: approximately 13% of U.S. Food and Drug Administration (FDA) approved drugs target nuclear hormone receptors.

BioInvenu has developed various NHR LinkLight™ assays. An inactive permuted luciferase containing a Tobacco Etch Virus (TEV) protease cleavage site is fused to a peptide containing NCOA-NHR interaction domain and a full-length NHR is fused to the TEV protease. Active luciferase is generated when the NCOA domain peptide-pLuc fusion protein interacts with the full-length NHR fused to TEV protease upon ligand activation.

NHR LinkLight™ assay offers a new cell-based screening method using full-length NHR protein in its native confirmation. In contrast to regulatory elements driving reporter gene expression assays that are prone to non-specific interference, the LinkLight™ assay generates immediate and specific signal readout. Compounds that activate NHRs, blocking NHR-ligand interaction, or modulate NHR conformation, resulting in signal alternation, could be identified using NHR LinkLight™ assay.

View our NHR LinkLight™ assay-ready cells.