Department of Medicinal Chemistry, Piramal Enterprises Ltd , 1, Nirlon Complex, Off Western Exp. Highway, Near NSE Complex, Goregaon East, Mumbai, Maharashtra 400 063 , India +91 22 30818078 ;
Expert Opin Ther Pat. 2013 Dec;23(12):1581-90. doi: 10.1517/13543776.2013.842977. Epub 2013 Oct 6.
Type 2 diabetes (T2D) is a complex metabolic disorder characterized by persistent hyperglycemia and a wide range of underlying metabolic defects. The prevalence and incidence of T2D are expected to dramatically increase in the near-future and consequently, there is a significant medical need for diabetes care. Many targets are under investigation to lower the plasma glucose levels or increase the insulin sensitivity. Despite newer drug classes emerging as viable long-term treatment options for the management of T2D, achieving an optimal glycemic control along with sufficient effectiveness over the course of the disease remains a challenge. In this regard, among several G-protein-coupled receptors (GPCRs), GPR120 and GPR40 have recently been considered as viable targets for diabetes and metabolic disorders.
This article reviews the current literature on the discovery and development of GPR120 agonists in diabetes and metabolic disorders and updates on the published patents in this field. The patent study for this review has been carried out using multiple electronic databases including SciFinder and Thomson Reuters Integrity.
A paradigm shift in the treatment of diabetes is needed, wherein a single therapeutic agent could target diabetes and its associated disorders such as high plasma glucose level and inflammation, with excellent safety and tolerability profile. In this regard, agonists of GPR120 or dual-agonist GPR120 and GPR40 are highly anticipated as therapeutic approaches for the treatment of diabetes on the basis of their novel glucose-dependent mechanism of action.
2 型糖尿病（T2D）是一种复杂的代谢紊乱，其特征是持续的高血糖和广泛的潜在代谢缺陷。预计 T2D 的患病率和发病率将在不久的将来大幅增加，因此对糖尿病治疗存在重大的医疗需求。许多靶点正在被研究用于降低血浆葡萄糖水平或提高胰岛素敏感性。尽管新兴的药物类别作为 T2D 管理的可行长期治疗选择出现，但在疾病过程中实现最佳血糖控制和足够的疗效仍然是一个挑战。在这方面，在几种 G 蛋白偶联受体（GPCR）中，GPR120 和 GPR40 最近被认为是糖尿病和代谢紊乱的可行靶点。
本文综述了 GPR120 激动剂在糖尿病和代谢紊乱中的发现和开发的最新文献，并更新了该领域已发表的专利。本综述的专利研究使用了多个电子数据库，包括 SciFinder 和 Thomson Reuters Integrity。
需要在糖尿病治疗方面进行范式转变，其中单一治疗剂可以针对糖尿病及其相关疾病，如高血糖和炎症，具有出色的安全性和耐受性。在这方面，基于其新颖的葡萄糖依赖性作用机制，GPR120 激动剂或双重激动剂 GPR120 和 GPR40 被高度期待作为治疗糖尿病的治疗方法。
