PPARgamma Human NHR Cell Based Antagonist Protein-Protein Interaction LeadHunter Assay - US

Background Information:

Peroxisomes proliferators include hypolipidemic drugs, leukotriene receptor antagonists and other materials.  The term is used because they induce an increase in the size and number of peroxisomes, which are subcellular organelles found in animals and plants that contain enzymes for respiration and for cholesterol and lipid metabolism.  The action of peroxisome proliferators is thought to be mediated via specific receptors, called PPARs, which belong to the steroid hormone receptor superfamily that function as transcription factors regulating the expression of genes.  All PPARs heterodimerase with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes.  PPARs play essential roles in the regulation of cellular differentiation, development, and metabolism (carbohydrate, lipid, protein) of higher organisms.  Three closely related subtypes (alpha, beta/delta, and gamma) have been identified.  PPARG (PPARγ) is expressed in three forms: γ1 is expressed in virtually all tissues including heart, muscle, colon, kidney, pancreas and spleen while γ2 is expressed mainly in adipose tissue liver, kidney, heart, muscle, adipose tissue and γ3 is expressed in macrophages, large intestine and white adipose tissue.  PPARG, stimulated by the drug class of thiazolidinediones (TZDs), is used in the treatment of diabetes mellitus and other diseases that feature insulin resistance; PPARG stimulation may also be used for the treatment of obesity, hypolipidemia and several cancers. Inhibition of PPARG may enhance tumorigenesis.

PathHunter NHR Protein Interaction cell lines are engineered to co-express a ProLink™ (PK) tagged NHR and an Enzyme Acceptor (EA) tagged SRC protein.  Activation of the receptor results in SRC-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK).  The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.

Family:

NHR

Sub Family:

Peroxisome Proliferator-Activated

Class:

Non-Steroid

Protein Name:

PPARgamma

Uniprot Number:

P37231

Protein Aliases:

Nuclear receptor subfamily 1 group C member 3

Gene Name:

PPARG

Gene ID:

5468

Gene Aliases:

PPARG1|PPARG2|NR1C3|PPARgamma

Accession Number:

NM_138711

Organism:

Human

Cell Type:

CHO-K1