PPARγ is a ligand-activated transcription factor involved in the regulation of lipid homeostasis and may function as a master regulator of adipogenesis.^1,2,3,4 Ligands for PPARγ include antidiabetic drugs of the thiazolidinedione structural class, 15-deoxy-Δ^12,14-prostaglandin J₂, and NSAIDS.^5,6,7,8 BADGE is a synthetic compound used in the production of polycarbonate and industrial plastics. This compound was recently identified as an antagonist of PPARγ.⁹ BADGE binds to PPARγ with an apparent K_d of 100 µM and interferes with the ability of 3T3-L1 and 3T3-F442A cells to undergo hormone-mediated cell differentiation.⁹

1 Elbrecht, A., Chen, Y., Cullinan, C.A., et al. Molecular cloning, expression and characterization of human peroxisome proliferator activated receptors γ 1 and γ 2. Biochem Biophys Res Commun 224 431-437 (1996).

2 Greene, M.E., Blumberg, B., McBride, O.W., et al. Isolation of the human peroxisome proliferator activated receptor γ cDNA: Expression in hematopoietic cells and chromosomal mapping. Gene Expr 4 281-299 (1995).

3 Spiegelman, B.M., and Flier, J.S. Adipogenesis and obesity: Rounding out the big picture. Cell 87 377-389 (1995).

4 Lemberger, T., Desvergne, B., and Wahli, W. Peroxisome proliferator-activated receptors: A nuclear receptor signaling pathway in lipid physiology. Annu Rev Cell Dev Biol 12 335-363 (1996).

5 Lehmann, J.M., Moore, L.B., Smith-Oliver, T.A., et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-acivated receptor γ (PPARγ). J Biol Chem 270 12953-12956 (1995).

6 Willson, T.M., Cobb, J.E., Cowan, D.J., et al. The structure-activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem 39 665-668 (1996).

7 Forman, B.M., Tontonoz, P., Chen, J., et al. 15-Deoxy-Δ^12,14-prostaglandin J₂ is a ligand for the adipocyte determination factor PPARγ. Cell 83 803-812 (1995).

8 Lehmann, J.M., Lenhard, J.M., Oliver, B.B., et al. Peroxisome proliferator-activated receptors a and g are activated by indomethacin and other non-steroidal anti-inflammatory drugs. J Biol Chem 272 3406-3410 (1997).

9 Wright, H.M., Clish, C.B., Mikami, T., et al. A synthetic antagonist for the peroxisome proliferator-activated receptor γ inhibits adipocyte differentiation. J Biol Chem 275 1873-1877 (2000).

Forman, B.M., Tontonoz, P., Chen, J., et al. 15-Deoxy-Δ^12,14-prostaglandin J₂ is a ligand for the adipocyte determination factor PPARγ. Cell 83 803-812 (1995).

Greene, M.E., Blumberg, B., McBride, O.W., et al. Isolation of the human peroxisome proliferator activated receptor γ cDNA: Expression in hematopoietic cells and chromosomal mapping. Gene Expr 4 281-299 (1995).

Lehmann, J.M., Lenhard, J.M., Oliver, B.B., et al. Peroxisome proliferator-activated receptors a and g are activated by indomethacin and other non-steroidal anti-inflammatory drugs. J Biol Chem 272 3406-3410 (1997).

Lemberger, T., Desvergne, B., and Wahli, W. Peroxisome proliferator-activated receptors: A nuclear receptor signaling pathway in lipid physiology. Annu Rev Cell Dev Biol 12 335-363 (1996).

Elbrecht, A., Chen, Y., Cullinan, C.A., et al. Molecular cloning, expression and characterization of human peroxisome proliferator activated receptors γ 1 and γ 2. Biochem Biophys Res Commun 224 431-437 (1996).

Spiegelman, B.M., and Flier, J.S. Adipogenesis and obesity: Rounding out the big picture. Cell 87 377-389 (1995).

Willson, T.M., Cobb, J.E., Cowan, D.J., et al. The structure-activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem 39 665-668 (1996).

Wright, H.M., Clish, C.B., Mikami, T., et al. A synthetic antagonist for the peroxisome proliferator-activated receptor γ inhibits adipocyte differentiation. J Biol Chem 275 1873-1877 (2000).

Lehmann, J.M., Moore, L.B., Smith-Oliver, T.A., et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-acivated receptor γ (PPARγ). J Biol Chem 270 12953-12956 (1995).

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BADGE is available in the following screening library:

• Bio-active Lipid I Screening Library (96-Well)