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MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edema.
Mol Endocrinol
July 2009
Metabolex, Department of Biology, Hayward, California 94545, USA.
MBX-102/JNJ39659100 (MBX-102) is in clinical development as an oral glucose-lowering agent for the treatment of type 2 diabetes. MBX-102 is a nonthiazolidinedione (TZD) selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-gamma that is differentiated from the TZDs structurally, mechanistically, preclinically and clinically. In diabetic rodent models, MBX-102 has insulin-sensitizing and glucose-lowering properties comparable to TZDs without dose-dependent increases in body weight.
View Article and Find Full Text PDFPPARgamma agonists attenuate proliferation and modulate Wnt/beta-catenin signalling in melanoma cells.
Int J Biochem Cell Biol
April 2009
The University of Queensland, Institute for Molecular Bioscience, Qld 4072, Australia.
Peroxisome proliferator-activated receptor-gamma (PPARgamma) is a member of the nuclear hormone receptor (NHR) superfamily of ligand-activated transcriptional regulators. Accumulating evidence suggests that PPARgamma agonists such as the thiazolidinediones (TZDs) may prove to be useful anti-cancer agents exhibiting anti-proliferative and/or pro-apoptotic affects in a range of cancer cell types including melanoma, however, the mechanisms underlying this effect remain unclear. We have demonstrated the anti-proliferative effects of full and partial PPARgamma modulators in human melanoma cell lines.
View Article and Find Full Text PDFSelective Modulators of PPAR-gamma Activity: Molecular Aspects Related to Obesity and Side-Effects.
PPAR Res
July 2011
Department of Biology, Metabolex Inc., 3876 Bay Center Place, Hayward, CA 94545, USA.
Peroxisome proliferator-activated receptor gamma (PPAR-gamma) is a key regulator of lipid metabolism and energy balance implicated in the development of insulin resistance and obesity. The identification of putative natural and synthetic ligands and activators of PPAR-gamma has helped to unravel the molecular basis of its function, including molecular details regarding ligand binding, conformational changes of the receptor, and cofactor binding, leading to the emergence of the concept of selective PPAR-gamma modulators (SPPARgammaMs). SPPARgammaMs bind in distinct manners to the ligand-binding pocket of PPAR-gamma, leading to alternative receptor conformations, differential cofactor recruitment/displacement, differential gene expression, and ultimately differential biological responses.
View Article and Find Full Text PDFHalofenate is a selective peroxisome proliferator-activated receptor gamma modulator with antidiabetic activity.
Diabetes
September 2006
Institute for Molecular Bioscience, University of Queensland, St. Lucia, Australia.
Halofenate has been shown previously to lower triglycerides in dyslipidemic subjects. In addition, significant decreases in fasting plasma glucose were observed but only in type 2 diabetic patients. We hypothesized that halofenate might be an insulin sensitizer, and we present data to suggest that halofenate is a selective peroxisome proliferator-activated receptor (PPAR)-gamma modulator (SPPARgammaM).
View Article and Find Full Text PDFHalofenate and clofibrate inhibition of pyruvate dehydrogenase from Fusarium culmorum.
J Environ Sci Health B
April 1985
Pyruvate dehydrogenase (E1, E.C. 1.
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