[HTML][HTML] An antidiabetic Thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor Γ (PPARγ)∗

…, TA Smith-Oliver, WO Wilkison, TM Willson… - Journal of Biological …, 1995 - ASBMB
Thiazolidinedione derivatives are antidiabetic agents that increase the insulin sensitivity of
target tissues in animal models of non-insulin-dependent diabetes mellitus. In vitro, …

The peroxisome proliferator-activated receptor-γ is a negative regulator of macrophage activation

M Ricote, AC Li, TM Willson, CJ Kelly, CK Glass - Nature, 1998 - nature.com
The peroxisome proliferator-activated receptor-γ (PPAR-γ) is a member of the nuclear receptor
superfamily of ligand-dependent transcription factors that is predominantly expressed in …

Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors α and γ

…, P Devchand, W Wahli, TM Willson… - Proceedings of the …, 1997 - National Acad Sciences
Peroxisome proliferator-activated receptors (PPARs) α and γ are key regulators of lipid
homeostasis and are activated by a structurally diverse group of compounds including fatty acids, …

Bile acids: natural ligands for an orphan nuclear receptor

…, TG Consler, SA Kliewer, JB Stimmel, TM Willson… - Science, 1999 - science.org
Bile acids regulate the transcription of genes that control cholesterol homeostasis through
molecular mechanisms that are poorly understood. Physiological concentrations of free and …

A prostaglandin J2 metabolite binds peroxisome proliferator-activated receptor γ and promotes adipocyte differentiation

SA Kliewer, JM Lenhard, TM Willson, I Patel, DC Morris… - Cell, 1995 - cell.com
Prostaglandins(PGs) of the Jz series form in vivo and exert effects on a variety of biological
processes. While most PGs mediate their effects through G protein-coupled receptors, the …

Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-γ

…, MH Lambert, R Kurokawa, MG Rosenfeld, TM Willson… - Nature, 1998 - nature.com
The peroxisome proliferator-activated receptor-γ (PPAR-γ) is a ligand-dependent transcription
factor that is important in adipocyte differentiation and glucose homeostasis and which …

The PPARs: from orphan receptors to drug discovery

TM Willson, PJ Brown, DD Sternbach… - Journal of medicinal …, 2000 - ACS Publications
Dietary fat intake is an environmental factor that affects many aspects of human health. 1
Several lines of evidence suggest that common diseases of modern society are associated with …

[PDF][PDF] A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis

…, MC Lewis, ME Roth, PR Maloney, TM Willson… - Molecular cell, 2000 - cell.com
Bile acids repress the transcription of cytochrome P450 7A1 (CYP7A1), which catalyzes the
rate-limiting step in bile acid biosynthesis. Although bile acids activate the farnesoid X …

The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.

…, DD McKee, MA Watson, TM Willson… - The Journal of …, 1998 - Am Soc Clin Investig
The cytochrome P-450 monooxygenase 3A4 (CYP3A4) is responsible for the oxidative
metabolism of a wide variety of xenobiotics including an estimated 60% of all clinically used drugs…

[HTML][HTML] An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway

…, SA Jones, DD McKee, BB Oliver, TM Willson… - Cell, 1998 - cell.com
Steroid hormones exert profound effects on differentiation, development, and homeostasis in
higher eukaryotes through interactions with nuclear receptors. We describe a novel orphan …