Indigo Biosciences, Inc. | Nuclear Receptor Reporter Gene Assays

Nuclear Receptor Reporter Gene Assays

Nuclear receptors (NRs) are a large class of ligand-inducible transcription factors. Many of these proteins comprise major drug targets that play key roles in cancer, diabetes, and other diseases. We offer high throughput cellular reporter gene assays for numerous nuclear receptors including:

Receptors		NCBI	Genecards	Geneatlas	Map
PPARalpha	Peroxisome proliferator-activated receptor-alpha	N	G	GA	M
PPARbeta	Peroxisome proliferator-activated receptor-beta	N	G	GA	M
PPARgamma	Peroxisome proliferator-activated receptor-gamma	N	G	GA	M
CAR	Constitutive androstane receptor	N	G	GA	M
FXR	Farnesoid X receptor	N	G	GA	M
RXRalpha	Retinoid X receptor-alpha	N	G	GA	M
ERRalpha	Estrogen related receptor-alpha	N	G	GA	M
TRalpha	Thyroid hormone receptor-alpha	N	G	GA	M
PR	Progesterone receptor	N	G	GA	M
ERalpha	Estrogen receptor-alpha	N	G	GA	M
ERbeta	Estrogen receptor-beta	N	G	GA	M
AR	Androgen receptor	N	G	GA	M
GR	Glucocorticoid receptor	N	G	GA	M
MR	Mineralocorticoid receptor	N	G	GA	M
LXRalpha	Liver X receptor-alpha	N	G	GA	M
LXRbeta	Liver X receptor-beta	N	G	GA	M
VDR	Vitamin D receptor	N	G	GA	M
RORalpha	RAR-related orphan receptor-alpha	N	G	GA	M

Representative examples of effects of small molecules on NR activity are shown below. Click the graphs to see a larger version.

References:

Vanden Heuvel, J.P. “Peroxisome Proliferator-Activated Receptors (PPARs) and Carcinogenesis” Toxicol. Sci. 1999, 47, 1-8.

Bility, M.T., Thompson, J.T., McKee, R.H., David, R.M., Butala, J.H., Vanden Heuvel, J.P., and Peters, J.M. “Activation of mouse and human peroxisome proliferator-activated receptors (PPARs) by phthalate monoesters.” Toxicol. Sci., 2004, 82, 170-182.

Muddana, S. S., Price A. M., MacBride, M. M. and Peterson, B. R. "11beta-Alkyl-Δ9-19-Nortestosterone Derivatives: High Affinity Ligands and Potent Partial Agonists of the Androgen Receptor " J. Med. Chem., 2004, 47, 4985-4988.

Yu, Y., Correll, P.H., and Vanden Heuvel, J.P. “Conjugated Linoleic Acid Decreases Production of Pro-inflammatory Products in Macrophages: Evidence for a PPARgamma-dependent Mechanism” Biochim. Biophys. Acta, 2002, 1581, 82-99.

Sumanasekera, W.K., Tien, E.S., Davis, J.W., Turpey, R., Perdew, G.H., and Vanden Heuvel, J.P. “Heat Shock Protein-90 (Hsp90) Acts as a Repressor of Peroxisome Proliferator-Activated Receptor-alpha (PPARalpha) and PPARbeta Activity” Biochem., 2003, 42, 10726-10735.