OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
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 heterodimerize 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, and muscle, and γ3 is expressed in macrophages, large intestine, and white adipose tissue. PPARγ, stimulated by the drug class of thiazolidinediones (TZDs), is used in the treatment of diabetes mellitus and other diseases that feature insulin resistance; PPARγ stimulation may also be used for the treatment of obesity, hyperlipidemia, and several cancers. PPARγ is also mildly stimulated by some NSAIDs (e.g., ibuprofen) and indoles. Inhibition of PPARγ may enhance tumorigenesis.
No. of Assays on Panel:
2
Assays on Panel:
Family
NHR
Name
PPARgamma Human NHR Functional Agonist Coactivator LeadHunter Assay - TW
Item
338240-0
Protein
PPARgamma
Organism
Human
Assay Sub Type
Protein-Protein Interaction
Family
NHR
Name
PPARgamma Human NHR Functional Antagonist Coactivator LeadHunter Assay - TW
Item
338240-1
Protein
PPARgamma
Organism
Human
Assay Sub Type
Protein-Protein Interaction
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_005037
Organism:
Human
Construct Details:
LBD, Recombinant
Assay Information
Assay Type:
Functional
Assay Sub Type:
Protein-Protein Interaction
Functional Mode:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant PPARγ receptors expressed in insect cells are used. Test compound and/or vehicle is incubated with the 2 nMǂ receptors and coactivator peptide for 180 minutes at room temperature. Determination of the amount of complex formed is read spectrofluorimetrically (excitation: 337 nm, emission: 520/490 nm). Test compound-induced increase fluorescence by 50 percent or more (≥50%) relative to 1 µM GW1929 response indicates possible PPARγ receptor agonist activity. Test compound-induced inhibition of 5 nM GW1929-induced fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
180 min. at 25°C
Control Inhibitor:
GW9662
Control Activator:
GW1929
Criteria For Significance:
≥ 50% increase in fluorescence relative to GW1929 response, ≥ 50% Inhibition of GW1929-induced fluorescnece
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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