摘要
背景:过氧化物酶体增殖物激活受体γ(PPARγ)是作为配体诱导转录因子的核受体超家族成员之一。它调节葡萄糖和脂质代谢,免疫,细胞生长和分化。噻唑烷二酮(TZDS)是一种有效的胰岛素增敏剂,通过激活PPAR发挥作用,对PPARγ具有较高的特异性。应付款为了保持胰岛β细胞功能和减少胰岛素抵抗,TZDs已经成为治疗2型糖尿病(T2D)的最常用的药物之一。椭圆形由美国食品和药物管理局(Fda)和首次使用于1997。 目的:然而,不良反应,包括体重增加,骨丢失,液体潴留,充血性心力衰竭,和膀胱癌的风险,削弱了TZDS在T2D治疗中的优势。那里因此,迫切需要对pPARγ表达和活性的调控机制有更深入的了解,以便新的pPARγ调节治疗学的种类少或弱。可以发挥作用。 结论:本文系统地综述了PPARγ的作用机制和多层调控机制。此外,新的治疗学类对pPARγ的调节作用以及对ge的新的研究方向。本文着重介绍了影响pPARγ功能和抗糖尿病药物反应的变异体,揭示了pPARγ是开发安全、精确药物治疗的一个有希望的靶点。策略( strategy的名词复数 ).
关键词: 过氧化物酶体增殖物激活受体γ,精密药物,新疗法,作用和调节机制,噻唑烷二酮,2型糖尿病。
Current Drug Targets
Title:Advances on PPARγ Research in the Emerging Era of Precision Medicine
Volume: 19 Issue: 6
关键词: 过氧化物酶体增殖物激活受体γ,精密药物,新疗法,作用和调节机制,噻唑烷二酮,2型糖尿病。
摘要: Background: Peroxisome proliferator-activated receptor gamma (PPARγ) is a member of the nuclear receptor superfamily that functions as a ligand-inducible transcription factor. It regulates glucose and lipid metabolism, immunity, and cellular growth and differentiation. Thiazolidinediones (TZDs) are potent insulin sensitizers that function by activating PPARs, with a high specificity for PPARγ. Due to their ability to preserve pancreatic beta cell function and reduce insulin resistance, TZDs have become one of the most prescribed classes of medications for type 2 diabetes (T2D) since their approval by the US Food and Drug Administration (FDA) and initial use in 1997.
Objective: However, adverse effects, including weight gain, bone loss, fluid retention, congestive heart failure, and risk to bladder cancer, have weakened the benefits of TZDs in T2D therapies. Therefore, there is an urgent need to have a deeper understanding of regulatory mechanisms of PPARγ expression and activity so that novel classes of PPARγ-modulating therapeutics with fewer or weaker side effects can be developed.
Conclusion: This article systematically reviews PPARγ's mechanisms of action and multilayer regulations. In addition, novel classes of therapeutics modulating PPARγ and new direction of research on genetic variants that affect PPARγ function and antidiabetic drug response are highlighted, which sheds light on PPARγ as a promising target for developing safer and precision medicine based therapeutic strategies.
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Cite this article as:
Advances on PPARγ Research in the Emerging Era of Precision Medicine, Current Drug Targets 2018; 19 (6) . https://dx.doi.org/10.2174/1389450118666170622091333
DOI https://dx.doi.org/10.2174/1389450118666170622091333 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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