Bile acid receptors as targets for drug development

FG Schaap, M Trauner, PLM Jansen - Nature reviews Gastroenterology …, 2014 - nature.com
The intracellular nuclear receptor farnesoid X receptor and the transmembrane G protein-
coupled receptor TGR5 respond to bile acids by activating transcriptional networks and/or …

Thiazolidinediones and the promise of insulin sensitization in type 2 diabetes

RE Soccio, ER Chen, MA Lazar - Cell metabolism, 2014 - cell.com
Type 2 diabetes is caused by insulin resistance coupled with an inability to produce enough
insulin to control blood glucose, and thiazolidinediones (TZDs) are the only current …

Glucocorticoids and fetal programming part 2: mechanisms

VG Moisiadis, SG Matthews - Nature Reviews Endocrinology, 2014 - nature.com
The lifelong health of an individual is shaped during critical periods of development. The
fetus is particularly susceptible to internal and external stimuli, many of which can alter …

AG protein-coupled receptor responsive to bile acids

Y Kawamata, R Fujii, M Hosoya, M Harada… - Journal of Biological …, 2003 - ASBMB
So far some nuclear receptors for bile acids have been identified. However, no cell surface
receptor for bile acids has yet been reported. We found that a novel G protein-coupled …

Activation of the aryl hydrocarbon receptor by structurally diverse exogenous and endogenous chemicals

MS Denison, SR Nagy - Annual review of pharmacology and …, 2003 - annualreviews.org
The induction of expression of genes for xenobiotic metabolizing enzymes in response to
chemical insult is an adaptive response found in most organisms. In vertebrates, the AhR is …

Vitamin E, antioxidant and nothing more

MG Traber, J Atkinson - Free radical biology and medicine, 2007 - Elsevier
All of the naturally occurring vitamin E forms, as well as those of synthetic all-rac-α-
tocopherol, have relatively similar antioxidant properties, so why does the body prefer α …

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

B Goodwin, SA Jones, RR Price, MA Watson… - 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 …

Role of LXRs in control of lipogenesis

JR Schultz, H Tu, A Luk, JJ Repa… - Genes & …, 2000 - genesdev.cshlp.org
The discovery of oxysterols as the endogenous liver X receptor (LXR) ligands and
subsequent gene targeting studies in mice provided strong evidence that LXR plays a …

Induction of phase I, II and III drug metabolism/transport by xenobiotics

C Xu, CYT Li, ANT Kong - Archives of pharmacal research, 2005 - Springer
Drug metabolizing enzymes (DMEs) play central roles in the metabolism, elimination and
detoxification of xenobiotics and drugs introduced into the human body. Most of the tissues …

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 …