以芳香烃受体为药物靶点的肿瘤治疗研究  

Anti-tumor therapy for targeting aryl hydrocarbon receptor

作　　者：刘颖[1] 张洪英[2] 唐涛[1] 刘飞飞[1] 吴谓[1] 罗瑛[1] 张继虹[1] 

机构地区：[1]昆明理工大学医学院衰老与肿瘤分子遗传学实验室,云南昆明650500 [2]寿光市人民医院羊口分院,山东寿光262714

出　　处：《中国药理学通报》2016年第5期607-612,共6页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 81260501);云南省应用基础研究计划项目(No 2014FD011)

摘　　要：芳香烃受体(aryl hydrocarbon receptor,AhR)是一种配体依赖性转录因子,可调控如2,3,7,8-四氯代苯并二恶英(2,3,7,8-tetrachlorodibenzo-p-dioxins,TCDDs)等外源性配体化合物的毒性作用。通过参与细胞增殖与凋亡、免疫代谢等过程,AhR影响肿瘤的生长、存活、迁移和侵袭。AhR对肿瘤的调控具有双重作用,在多环芳烃、卤代芳烃等配体作用下,AhR可促进肿瘤生成;但苯并噻唑、氨基黄酮等化合物激活AhR后,可发挥抑癌功能,有望成为治疗肿瘤的药物靶点。该文主要讨论AhR在肿瘤中的作用、以AhR为靶点的药物作用机制以及目前AhR靶向药物的研究现状。Aryl hydrocarbon receptor ( AhR) is a ligand-depend-ent transcription factor that mediates the toxicity of xenobiotic ligands like 2,3,7,8-tetrachlorodibenzo-p-dioxins(TCDDs). AhR influences tumor growth, survival, migration and invasion by regulating proliferation, apoptosis and immune metabolism of tumor cells. AhR has two ways to regulate tumor development, and ligands like polycyclic aromatic hydrocarbons( PAHs) , hal-ogenated aromatic hydrocarbons( HAHs) can induce tumorigene-sis. However, some compounds such as benzothiazole and amin-oflavone can activate AhR, which suppresses the tumor progres-sion and suggests that AhR may be a novel drug target for anti-tumor therapy. The paper discussed the role of AhR in tumori-genesis, the mechanism of the drugs targetting AhR and the sta-tus of studying AhR as a potential target in anticancer therapy.

关 键 词：芳香烃受体 肿瘤 配体 靶向药物 作用机制 研究现状 

分 类 号：R-05[医药卫生] R329.11