Induction of Drug Metabolism¶
Handschin, & Meyer. (2003). Induction of Drug Metabolism: The Role of Nuclear Receptors.
Cited by¶
1 citation across 1 artifact.
Each citation links to the sentence it supports in the citing article.
Domain-specific¶
- Enzyme Induction
- The mechanism operates through ligand-activated nuclear transcription factors: the xenobiotic binds a receptor such as PXR (pregnane X receptor), CAR (constitutive androstane receptor), or AhR (aryl hydrocarbon receptor); the ligand-bound receptor translocates to the nucleus and binds cognate response elements on target gene promoters; the resulting increase in transcription raises expression of specific cytochrome P450 isoforms (most prominently CYP3A4, CYP2B6, CYP1A2) and phase-II conjugation enzymes, enlarging the enzymatic pool available to process substrates
This sourceHandschin and Meyer's review of drug-metabolism induction places the xenobiotic-sensing nuclear receptors PXR and CAR, acting as RXR heterodimers, at response elements in the regulatory regions of the induced genes. Handschin and Meyer's review notes that PXR is directly activated by xenobiotic ligands whereas CAR is engaged by a more complex and less well understood signalling route.
Supported in partVerified against a saved copy of the source
“the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR), two members of the nuclear receptor superfamily of transcription factors, were discovered to act as sensors for lipophilic xenobiotics”
- The mechanism operates through ligand-activated nuclear transcription factors: the xenobiotic binds a receptor such as PXR (pregnane X receptor), CAR (constitutive androstane receptor), or AhR (aryl hydrocarbon receptor); the ligand-bound receptor translocates to the nucleus and binds cognate response elements on target gene promoters; the resulting increase in transcription raises expression of specific cytochrome P450 isoforms (most prominently CYP3A4, CYP2B6, CYP1A2) and phase-II conjugation enzymes, enlarging the enzymatic pool available to process substrates
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Registry ID ref:71484a543484 · see in the full table