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Structure and function research of the nuclear receptor PPARγ and its novel selective regulator

Abstract

过氧化物酶体增殖剂激活受体家族(PPARs)是一类配体依赖型的激活因子,它们是核受体超家族中的重要成员。PPARs是机体调节新陈代谢平衡的关键转录因子,因此PPARs也成为了研发治疗糖尿病,心血管疾病等代谢相关疾病药物的热门分子靶标。 糖尿病是困扰现代人健康的一组常见代谢性疾病,但是目前临床上仍然缺乏安全且有效的糖尿病治疗药物。噻唑烷二酮(Thiazolidinedione,TZD)类药物是经典的PPARγ完全激动剂,由于它能够改善由糖尿病引起的胰岛素耐受等症状,目前已经运用于临床治疗Ⅱ型糖尿病。但是TZDs在发挥抗糖尿病功效的同时也伴有严重的副作用,比如肝毒性、水肿、体重增加、骨质疏松和心...The PPARs belong to the nuclear receptor superfamily, a kind of transcription factors which most are ligand-inducible. PPARs are the most important regulators of the metabolic homeostasis, and they have gained a lot of interest as drug targets for cardiovascular disease, diabetes and so on. Type 2 diabetes mellitus (T2DM) is a prevalent metabolic syndrome that is characterized by insulin resista...学位:理学博士院系专业:生命科学学院_生物化学与分子生物学学号:2162013015413

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