The expression of drug-metabolizing enzymes when responding to stimulus signals is tightly regulated by a variety of transcription factors, including the nuclear receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR). These receptors are xenobiotic sensors that respond to environmental stimuli. The quest to understand the molecular mechanisms by which PXR and CAR control the expression of drug-metabolizing enzymes, including cytochrome P450s (P450s), has been one of the driving forces that established the current foundation of knowledge on the regulation of drug metabolism and disposition.

The special section on Drug Metabolism and Regulation found in Drug Metabolism and Disposition July 2022 (50/7) issue addresses the fundamental knowledge by the 2016 Bernard B. Brodie Award recipient Dr. Masahiko Negishi’s former mentor and trainees.

All content in the special section is freely accessible through February 2023.