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FFA1 (GPR40) Receptor Agonists Based on Phenylpropanoic Acid as Hypoglycemic Agents: Structure–Activity Relationship
Russian Journal of Bioorganic Chemistry ( IF 1 ) Pub Date : 2020-12-28 , DOI: 10.1134/s1068162020060151
S. O. Kuranov , O. A. Luzina , N. F. Salakhutdinov

Abstract

Free fatty acid receptor-1 (FFA1) agonists have been considered for a long time as a potentially new class for the treatment of type 2 diabetes mellitus. Phenylpropanoic acid is the preferred scaffold in the development of FFA1 receptor agonists. This review analyzes the effect of structural fragments of phenylpropanoic acid-based agonists on receptor affinity, selectivity, biocompatibility, and metabolic stability. Current trends in the design of FFA1 receptor agonists are discussed.



中文翻译:

基于苯基丙酸作为降血糖药的FFA1(GPR40)受体激动剂:结构与活性的关系

摘要

长期以来,游离脂肪酸受体1(FFA1)激动剂被认为是治疗2型糖尿病的潜在新类别。苯丙酸是FFA1受体激动剂开发中的首选支架。这篇综述分析了基于苯丙酸的激动剂的结构片段对受体亲和力,选择性,生物相容性和代谢稳定性的影响。讨论了FFA1受体激动剂设计的当前趋势。

更新日期:2020-12-28
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