Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human

IF 2.3 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2020-03-01 Epub Date: 2019-12-27 DOI:10.1016/j.bmcl.2019.126857

Lian Zhu Liu , Tianwei Ma , Jingye Zhou , Zhi Long Hu , Xue Jun Zhang , Hai Zhen Zhang , Mi Zeng , Jia Liu , Lei Li , Yi Jiang , Zack Zou , Fan Wang , Lei Zhang , Jianfeng Xu , Jingru Wang , Fei Xiao , Xiankang Fang , Haixia Zou , Alexander M. Efanov , Melissa K Thomas , Jiehao Chen

引用次数: 4

Abstract

The discovery and optimization of a novel series of GPR142 agonists are described. These led to the identification of compound 21 (LY3325656), which demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. Compound 21 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.

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适合人临床试验的GPR142激动剂LY3325656的发现

本文描述了一系列新型GPR142激动剂的发现和优化。这导致了化合物21 (LY3325656)的鉴定，该化合物在临床前研究中显示出抗糖尿病作用，并且ADME/PK特性适合人体给药。化合物21是首个用于治疗2型糖尿病的GPR142激动剂分子。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.