Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Czech Republic.
Curr Drug Metab. 2011 Feb;12(2):198-212. doi: 10.2174/138920011795016818.
Aryl hydrocarbon receptor (AhR) is an important transcriptional regulator of drug metabolizing enzymes that dominantly controls the expression of cytochrome P450 CYP1 family genes and some phase II enzymes. AhR also has many endogenous functions including cell cycle control, immune response, and cell differentiation. In addition, AhR is well-known to be involved in chemically-induced carcinogenesis. AhR is activated by a variety of endogenous and exogenous ligands. While exogenous activation of AhR has deleterious effects on human organism, sustained activation of AhR by endogenous ligands is indispensable for proper cell functions. Therefore, the effects of exogenous and endogenous ligands on AhR resemble the Dr. Jekyll and Mr. Hyde story. The aim of the current paper is to summarize and update the knowledge on exogenous and endogenous AhR ligands.
芳香烃受体 (AhR) 是一种重要的转录调节因子,可调控药物代谢酶的表达,主要控制细胞色素 P450 CYP1 家族基因和一些 II 相酶的表达。AhR 还具有许多内源性功能,包括细胞周期控制、免疫反应和细胞分化。此外,AhR 还与化学诱导的致癌作用有关。AhR 可被多种内源性和外源性配体激活。虽然外源性激活 AhR 对人体有有害影响,但内源性配体持续激活 AhR 对于细胞的正常功能是不可或缺的。因此,外源性和内源性配体对 AhR 的影响类似于 Dr. Jekyll and Mr. Hyde 的故事。本文旨在总结和更新有关 AhR 外源性和内源性配体的知识。