Nuclear Receptor Screening

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 screening (HTS) using cellular reporter gene assays for numerous nuclear receptors including:

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

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.

    • Please contact an INDIGO representative for a quote with current pricing, turn-around time and report format at
    (814) 234-1919, or customerserv@indigobiosciences.com