PPAR-gamma

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Human PPAR-gamma (grey) complex with NCOA-1 peptide (green) and anti-diabetic agent (PDB code 3et3)

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3D structures of PPAR

Peroxisome Proliferator-Activated Receptors

Additional Resources

For additional information See: Diabetes
For additional information See: Regulation of Gene Expression
For additional information See: Peroxisome Proliferator-Activated Receptors

References

[1] Gampe Jr RT, Montana VG, Lambert MH, et al. Asymmetry in the PPARγ/RXRα crystal structure reveals the molecular basis of heterodimerization among nuclear receptors (2000) Molecular Cell, 15(9), pp.545-555.

[2] Zieleniak A, Wójcik M, Woźniak LA. Structure and physiology functions of the human peroxisome proliferator-activated receptor γ (2008) Arch. Immunol. Ther. Exp., 56 (5), pp. 331-345.

[3] Tontonoz P, Spiegelman BM. Fat and Beyond: The Diverse Biology of PPARγ (2008) Annu. Rev. Biochem., 77, pp. 289-312.

[4] Desvergne B, Wahli W. Peroxisome proliferator-activated receptors: Nuclear control of metabolism (1999) Endocrine Reviews, 20 (5), pp. 649-688.

[5] Lewis SN, Bassaganya-Riera J, Bevan DR. Virtual Screening as a Technique for PPAR Modulatory Discovery (2010) PPAR Research, 2010, pp. 861238.

[6] Itoh T, Fairall L, Amin K, et al. Structural basis for the activation of PPARγ by oxidized fatty acids (2008) Nature Structural and Molecular Biology, 15 (9), pp.924-931.

[7] Pochetti G, Godio C, Mitro N, et al. Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor γ ligand-binding domain in the complex with two enantiomeric ligands (2007) Journal of Biological Chemistry, 282 (23), pp.17314-17324.

[8] Murphy GJ, Holder JC. PPAR-γ agonists: Therapeutic role in diabetes, inflammation and cancer (2000) Trends in Pharmacological Sciences, 21 (12), pp. 469-474.

[9] Xu HE, Stanley TB, Montana VG, et al. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα (2002) Nature, 415 (6873), pp.813-817.

[10] Kallenberger BC, Love, JD, Chatterjee VKK, Schwabe JWR. A dynamic mechanism of nuclear receptor activation and its perturbation in a human disease (2003) Nature, 10 (2), pp.136-140.

[11] Shao D, Rangwala SM, Bailey ST, Krakow SA, Reginato MJ, Lazar MA. Interdomain communication regulating ligand binding by PPARγ (1998) Nature, 396, pp. 377-380.

[12] Su CG, Wen X, Bailey ST, Jiang W, Rangwala SM, Keilbaugh SA, Flanigan A, Murthy S, Lazar MA, Wu GD. A Novel therapy for colitis utilizing PPAR-γ ligands to inhibit the epithelial inflammatory response (1999) J Clin Invest., 104(4), pp. 383-389.

[13] Dubuquoy L, Rousseaux C, Thuru X, Peyrin-Biroulet L, Romano O, Chavatte P, Chamaillard M, Desreumaux P. PPARγ as a new therapeutic target in inflammatory bowel disease (2006) International Journal of Gastroenterology and Hepatology, 55 (9), pp.1341-1349.

[14] McKenna NJ, O'Malley BW. Combinatorial control of gene expression by nuclear receptors and coregulators (2002) Cell, 108 (4), pp. 465-474.

[15] Sartor, RB. Mechanisms of disease: pathogenesis of Crohn’s disease and ulcerative colitis (2006) Nature, 3(7), pp. 390-407.

[16] Aprahamian T, Bonegio RG, Richez C, Yasuda K, Chiang L, Sato K, Walsh K, Rifkin IR. The Peroxisome Proliferator-Activated Receptor γ Agonist Rosiglitazone Ameliorates Murine Lupus by Induction of Adiponectin (2009) the Journal of Immunology, 182, pp. 340 -346.

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