Novel Peptides as GIPR/GLP-1R/GCGR Triagonists for Treating Type 2 Diabetes Mellitus

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-07-31 DOI:10.1021/acsmedchemlett.5c00435

Qilong Hu, and , Steven H. Liang*,

引用次数: 0

Abstract

This patent application pertains to a novel class of peptide triagonists, generally represented by Formula I. These peptides exhibit selective activities toward GIPR (gastric inhibitory polypeptide receptor), GLP-1R (glucagon-like peptide-1 receptor), and GCGR (glucagon receptor). The unique pharma-cological profile of these triagonists offers promising therapeutic potential for the management of various conditions, including type 2 diabetes mellitus (T2DM), weight management, nonalcoholic fatty liver disease, etc.

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新型多肽作为GIPR/GLP-1R/GCGR三角激动剂治疗2型糖尿病

本专利申请涉及一类新型肽三角剂，通常由式1表示。这些肽对胃抑制性多肽受体（GIPR）、胰高血糖素样肽-1受体（GLP-1R）和胰高血糖素受体（GCGR）具有选择性活性。这些三角拮抗剂独特的药理学特征为各种疾病的治疗提供了有希望的治疗潜力，包括2型糖尿病（T2DM）、体重控制、非酒精性脂肪性肝病等。

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

ACS Medicinal Chemistry Letters CHEMISTRY, MEDICINAL-

CiteScore

7.30

自引率

2.40%

发文量

328

审稿时长

1 months

期刊介绍： ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to: Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics) Biological characterization of new molecular entities in the context of drug discovery Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc. Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic Mechanistic drug metabolism and regulation of metabolic enzyme gene expression Chemistry patents relevant to the medicinal chemistry field.