Abstract P-glycoprotein (P-gp) is an ATP-dependent efflux pump encoded by the MDR1
gene in humans, known to mediate multidrug resistance of neoplastic cells to cancer …

In this issue of Structure, Holmes et al.(2005) describe elements of an innate defense
mechanism that provides mammals a means to restrict bacterial growth. The host protein …

To commemorate the 50th anniversary of the Society of Toxicology, this special edition
article reviews the history and current scope of xenobiotic metabolism and transport, with …

Abstract The cytochrome P450 (P450) enzymes first attracted interest because of their
relevance to the metabolism of drugs, steroids, and carcinogens. Collectively, the 57 human …

Drug-metabolizing enzymes (DMEs) and transporters play pivotal roles in the disposition
and detoxification of numerous foreign and endogenous chemicals. To accommodate …

As a promiscuous xenobiotic sensor, pregnane X receptor (PXR) plays a crucial role in drug
metabolism. Since dietary phytochemicals exhibit the potential to modulate human PXR, this …

Purpose Interest in the use of herbal products has grown dramatically in the Western world.
Recent estimates suggest an overall prevalence for herbal preparation use of 13% to 63 …

The xenobiotic receptors CAR and PXR constitute two important members of the NR1I
nuclear receptor family. They function as sensors of toxic byproducts derived from …

Nuclear receptors (NRs) comprise a family of ligand inducible transcription factors. To
achieve transcriptional activation of target genes, DNA-bound NRs directly recruit general …

Induction of drug metabolism was described more than 40 years ago. Progress in
understanding the molecular mechanism of induction of drug-metabolizing enzymes was …