RORγt反向激动剂用于自身免疫性疾病治疗的研究进展
Progress in discovery of RORγt inverse agonists for the treatment of autoimmune diseases
鲁丽雪 1王永辉1
作者信息
- 1. 复旦大学药学院药物化学系, 上海 201203
- 折叠
摘要
视黄酸受体相关孤儿受体RORγt作为Th17细胞特异性转录因子可诱导Th17细胞的分化以及炎性因子IL-17等的产生,在炎症和自身免疫性疾病等病症的发生和发展过程中发挥着重要作用.近年来RORγt反向激动剂已成为学术界乃至国际制药公司研究的热点领域.目前已报道多种骨架结构类型,包括正构位点反向激动剂和变构位点反向激动剂.本文通过介绍RORγt的结构与功能,并对处于临床和临床前研究中的一些RORγt反向激动剂进行综述,以期为RORγt反向激动剂的进一步研究与开发提供参考.
Abstract
As a Th17 cell-specific transcription factor,retinoic acid receptor-related orphan receptor γt(RORγt),can induce differentiation of Th17 cells and production of inflammatory factor IL-17,playing an important role in inflammation and autoimmune diseases.RORγt inverse agonists have become a research hotspot in both academia and pharmaceutical companies around the world in recent years,with great development potential.A variety of skeletal structure types have been reported,including orthosteric and allosteric inverse agonists.In this paper,the structure and functions of RORγt are introduced,and RORγt inverse agonists in clinical and preclinical studies are reviewed in order to provide reference for further research and development of RORγt inverse agonists.
关键词
自身免疫性疾病/Th17细胞/RORγt反向激动剂Key words
autoimmune diseases/Th17 cells/RORγt inverse agonists引用本文复制引用
基金项目
国家自然科学基金(81874287)
上海市生物医药科技支撑计划项目(19431900100)
出版年
2024
国家科技期刊平台
NSTL
万方数据