芳基烃受体及其多种配体和功能:一种暴露体受体。

IF 11.2 1区 医学 Q1 PHARMACOLOGY & PHARMACY Annual review of pharmacology and toxicology Pub Date : 2022-01-06 Epub Date: 2021-09-09 DOI:10.1146/annurev-pharmtox-052220-115707
Lucie Larigot, Louise Benoit, Meriem Koual, Céline Tomkiewicz, Robert Barouki, Xavier Coumoul
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引用次数: 27

摘要

芳烃受体(AhR)是一种转录因子,在被多种配体激活后调节多种功能,包括外源生物、天然产物、微生物代谢产物和内源性分子。由于这种多样性,AhR构成了一个暴露体受体。它的主要功能之一是调节几种防御化学物质和细菌感染的防线。事实上,它除了具有良好的解毒功能外,还具有多种生理屏障功能,并在免疫调节中起着关键作用。AhR还参与了几个器官的发育及其体内平衡的维持。它的活性取决于配体的类型和受体激活的时间框架,这可以是持续的或短暂的,在某些情况下导致相反的调节模式,如不同癌症途径的调节所示。选择性调节剂的开发及其药理特性是研究的重要领域。
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Aryl Hydrocarbon Receptor and Its Diverse Ligands and Functions: An Exposome Receptor.

The aryl hydrocarbon receptor (AhR) is a transcriptional factor that regulates multiple functions following its activation by a variety of ligands, including xenobiotics, natural products, microbiome metabolites, and endogenous molecules. Because of this diversity, the AhR constitutes an exposome receptor. One of its main functions is to regulate several lines of defense against chemical insults and bacterial infections. Indeed, in addition to its well-established detoxication function, it has several functions at physiological barriers, and it plays a critical role in immunomodulation. The AhR is also involved in the development of several organs and their homeostatic maintenance. Its activity depends on the type of ligand and on the time frame of the receptor activation, which can be either sustained or transient, leading in some cases to opposite modes of regulations as illustrated in the regulation of different cancer pathways. The development of selective modulators and their pharmacological characterization are important areas of research.

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来源期刊
CiteScore
27.80
自引率
0.00%
发文量
53
期刊介绍: Since 1961, the Annual Review of Pharmacology and Toxicology has been a comprehensive resource covering significant developments in pharmacology and toxicology. The journal encompasses various aspects, including receptors, transporters, enzymes, chemical agents, drug development science, and systems like the immune, nervous, gastrointestinal, cardiovascular, endocrine, and pulmonary systems. Special topics are also featured in this annual review.
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