Abstract The amphetamine derivative (±)-3, 4-methylenedioxymethamphetamine (MDMA,
ecstasy) is a popular recreational drug among young people, particularly those involved in …

The human CYP3A subfamily plays a dominant role in the metabolic elimination of more
drugs than any other biotransformation enzyme. CYP3A enzyme is localized in the liver and …

The nuclear pregnane X receptor (PXR; NR1I2) is an important component of the body's
adaptive defense mechanism against toxic substances including foreign chemicals …

Novel immune checkpoint blockade with ipilimumab, an antibody blocking the cytotoxic T-
lymphocyte antigen 4 (CTLA4), is revolutionizing cancer therapy. However, ipilimumab …

▪ Abstract The metabolic nuclear receptors act as metabolic and toxicological sensors,
enabling the organism to quickly adapt to environmental changes by inducing the …

Many orally administered drugs must overcome several barriers before reaching their target
site. The first major obstacle to cross is the intestinal epithelium. Although lipophilic …

Nuclear receptors are transcription factors which sense changing environmental or
hormonal signals and effect transcriptional changes to regulate core life functions including …

The calcineurin inhibitors ciclosporin (cyclosporine) and tacrolimus are immunosuppressant
drugs used for the prevention of organ rejection following transplantation. Both agents are …

Mechanisms that protect the body from a diverse array of harmful chemicals are also
involved in drug metabolism, and can cause adverse drug–drug interactions. Two closely …

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 …