Discovering the potential of your compound to effect gene expression
Nuclear hormone receptors (NHRs) are a large superfamily of ligand-activated transcription factors that consist of two subtypes, steroid and non-steroid. These receptors serve as on-off switches for genes which regulate cell differentiation, proliferation, and metabolism, and thus can play a role in the pathology of cancer, cardiovascular disease, inflammation, and reproduction. As with many receptors, ligand binding induces a conformational change in the receptor, but unique to nuclear receptors is their ability to up- or down-regulate gene expression. This ability makes nuclear receptors interesting therapeutic and liability targets.
Eurofins offers a broad portfolio of both binding and functional assays, including co-activator recruitment for nuclear receptors. These assays can help provide a complete profile of your drug or compound and give you a better sense of its gene-regulating features.
Advantages of nuclear receptor profiling:
Figures 1. Activation and inhibition of human estrogen receptor, ERβ
The indicated reference compounds were tested in dose response for their ability to either activate (left panel) or inhibit (right panel) human estrogen receptor, ERβ, as detected by measuring the amount of coactivator recruitment.