Pregnane X receptor is involved in drug metabolism as a key regulator of CYP3A expression
- VernacularTitle:孕烷X受体对CYP3A基因表达的调控作用及其在药物代谢中的意义
- Author:
Dexiang XU
;
Wei WEI
- Publication Type:Journal Article
- Keywords:
cytochrome P4503A;
pregnane X receptor;
drug metabolism
- From:
Chinese Pharmacological Bulletin
1986;0(06):-
- CountryChina
- Language:Chinese
-
Abstract:
Cytochrome P4503As(CYP3As),the liver microsomal enzymes responsible for oxidative metabolism of numerous clinically used drugs,is known to be induced by a variety of compounds,including naturally occurring and synthetic glucocorticoids,pregnane compounds,and macrolide antibiotics.The pregnane X receptor(PXR;NR1I2) is an important component of the body′s adaptive defense against xenobiotics including drugs.PXR is activated by a large number of endogenous and exogenous chemicals including steroids,antibiotics,antimycotics,bile acids,and the herbal antidepressant St.John′s wort.PXR binds as a heterodimer with the 9-cis retinoic acid receptor(NR2B) to DNA response elements in the regulatory regions of CYP3A genes.Although PXR evolved to protect the body,its activation by a variety of prescription drugs represents the molecular basis for an important class of harmful drug interactions.
