Nuclear receptors and the regulation of drug‐metabolizing enzymes and drug transporters: implications for interindividual variability in response to drugs

BL Urquhart, RG Tirona, RB Kim - The Journal of Clinical …, 2007 - Wiley Online Library
Erratic or unpredictable response to drugs remains a challenge of modern drug therapy. An
important determinant of such interindividual differences in drug response is variability in the …

Nuclear receptors CAR and PXR: Molecular, functional, and biomedical aspects

A Di Masi, E De Marinis, P Ascenzi, M Marino - Molecular aspects of …, 2009 - Elsevier
Nuclear receptors (NRs) are ligand-activated transcription factors sharing a common
evolutionary history and having similar sequence features at the protein level. Selective …

CYP2B6: new insights into a historically overlooked cytochrome P450 isozyme

H Wang, LM Tompkins - Current drug metabolism, 2008 - ingentaconnect.com
Human CYP2B6 has been thought to account for a minor portion (< 1%) of total hepatic
cytochrome P450 (CYP) content and to have a minor function in human drug metabolism …

Nuclear receptors PXR and CAR: implications for drug metabolism regulation, pharmacogenomics and beyond

X Chai, S Zeng, W **e - Expert opinion on drug metabolism & …, 2013 - Taylor & Francis
Introduction:'Orphan'nuclear receptors belong to the nuclear receptor (NR) superfamily of
transcriptional factors. Binding of ligands to these receptors results in the recruitment of the …

PPARA: A Novel Genetic Determinant of CYP3A4 In Vitro and In Vivo

K Klein, M Thomas, S Winter, AK Nussler… - Clinical …, 2012 - Wiley Online Library
Interindividual variability in cytochrome P450 3A4 (CYP3A4) is believed to be largely
heritable; however, predictive genetic factors have remained scarce. Using a candidate …

Small-molecule modulators of PXR and CAR

SC Chai, MT Cherian, YM Wang, T Chen - Biochimica et Biophysica Acta …, 2016 - Elsevier
Two nuclear receptors, the pregnane X receptor (PXR) and the constitutive androstane
receptor (CAR), participate in the xenobiotic detoxification system by regulating the …

Why we need to take a closer look at genetic contributions to CYP3A activity

Q Zhai, M van der Lee, T van Gelder… - Frontiers in …, 2022 - frontiersin.org
Cytochrome P450 3A (CYP3A) subfamily enzymes are involved in the metabolism of 40% of
drugs in clinical use. Twin studies have indicated that 66% of the variability in CYP3A4 …

Human cytochrome P450 epoxygenases: variability in expression and role in inflammation-related disorders

P Shahabi, G Siest, UA Meyer… - Pharmacology & …, 2014 - Elsevier
Beyond their contribution to the metabolism of xenobiotics, cytochrome P450 (CYP)
epoxygenases are actively involved in the metabolism of endogenous substances, like …

Pathway-targeted pharmacogenomics of CYP1A2 in human liver

K Klein, S Winter, M Turpeinen, M Schwab… - Frontiers in …, 2010 - frontiersin.org
The human drug metabolizing cytochrome P450 (CYP) 1A2, is one of the major P450
isoforms contributing by about 5–20% to the hepatic P450 pool and catalyzing oxidative …

Nuclear receptor-mediated induction of CYP450 by antiretrovirals: functional consequences of NR1I2 (PXR) polymorphisms and differential prevalence in whites and …

J Svaerd, JP Spiers, F Mulcahy… - JAIDS Journal of …, 2010 - journals.lww.com
Background: Antiretroviral therapy including HIV protease inhibitors and nonnucleoside
reverse transcriptase inhibitors can both inhibit and induce expression of cytochrome P450s …