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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Indole scaffolds as a promising class of the aryl hydrocarbon receptor ligands
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Indole scaffolds as a promising class of the aryl hydrocarbon receptor ligands

机译：吲哚支架作为芳基烃受体配体的有希望的类别

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摘要

The aryl hydrocarbon receptor (AhR), deemed initially as a xenobiotic sensor, plays multiple physiological roles and is involved in various pathophysiological processes and many diseases' etiology. Therefore, the therapeutic and chemopreventive targeting of AhR is a fundamental issue. To date, thousands of structurally diverse ligands of AhR have been identified. The bottleneck in targeting the AhR is that it is a Janus-faced player with beneficial vs. harmful effects in the ligand-specific context. A distinct structural class of the AhR ligands is those with indole-based scaffolds. The present review summarizes the knowledge on the existing indole-derived AhR ligands, comprising natural and dietary compounds, synthetic compounds including clinically used drugs, endogenous intermediary metabolites, and catabolites produced by human microbiota. The examples of novel, indole ring containing, rational design based AhR ligands are presented. The molecular, in vitro, and in vivo effects are described. (C) 2021 Elsevier Masson SAS. All rights reserved.
机译：芳香烃受体（AhR）最初被认为是一种外源性传感器，发挥着多种生理作用，参与多种病理生理过程和多种疾病的病因。因此，针对AhR的治疗和化学预防是一个基本问题。迄今为止，已鉴定出数千种结构多样的AhR配体。针对AhR的瓶颈在于，它是一个面对Janus的参与者，在特定配体的环境中具有有利和有害的影响。AhR配体的一个独特结构类别是那些以吲哚为基础的支架。本综述总结了现有吲哚衍生AhR配体的知识，包括天然和膳食化合物、合成化合物（包括临床使用的药物）、内源性中间代谢物和人类微生物群产生的分解代谢产物。给出了基于合理设计的新型含吲哚环AhR配体的实例。描述了分子、体外和体内效应。（c）2021爱思唯尔马松SAS。版权所有。

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