二噁英受体的配体多样性研究进展

Research progress on ligand diversity of aryl hydrocarbon receptor

二噁英受体(AHR)是一种依赖于配体激活的转录因子,在细胞增殖与分化、细胞凋亡、癌细胞迁移以及炎症反应等多种生物学过程中具有至关重要的作用。AHR的激活依赖于外界环境中的多种有毒化合物或内源性配体的结合,不同类型配体通过激活AHR的不同信号通路发挥不同的功能。对不同结合位点的AHR配体分子进行归纳、总结,并对几类典型的激动剂和拮抗剂激活AHR的机制及其在不同疾病中的潜在毒理作用进行综述。深入了解AHR的激活机制及其毒理作用将有助于预防和治疗环境污染物所导致的疾病,并为以AHR为靶点的药物开发提供一定的理论指导。

Aryl hydrocarbon receptor(AHR)is a ligand-dependent activated transcription factor with critical roles in a variety of biological processes,including cell proliferation,differentiation,apoptosis,cancer migration and inflammation.The activation of AHR depends on the binding of various toxic compounds in the external environment or endogenous ligands.Different types of ligands mediate different signaling pathways of AHR and perform different functions.In this paper,the AHR ligands with different binding sites was concluded,and the molecular mechanisms of AHR activation by several typical agonists and antagonists were summarized.Furthermore,the potential toxicological effects in different diseases and tumors were reviewed.An in-depth understanding of the activation mechanisms and toxicological effects of AHR will help prevent and treat the development of diseases caused by environmental pollutants and provide some theoretical guidance for the development of drugs targeting AHR.