{"title":"Evolution and therapeutic potential of glucagon-like peptide 2 analogs","authors":"Binbin Gong , Ting Wang , Lidan Sun","doi":"10.1016/j.bcp.2025.116758","DOIUrl":null,"url":null,"abstract":"<div><div>Glucagon-like peptide 2 (GLP-2) is a proglucagon-derived peptide released by intestinal endocrine cells. However, its therapeutic potential is limited by rapid inactivation via dipeptidyl peptidase-IV. The elucidation of three-dimensional structures of G-protein-coupled receptors, including GLP-2 receptor, has facilitated the rational design of novel peptide therapeutics. Recent studies have explored various structural modifications based on the structure of GLP-2, such as amino acid substitution, lipidation, and fusion with proteins, to extend the half-life of GLP-2 and enhance its biological activity. One promising avenue involves the development of multifunctional molecules targeting multiple pharmacological systems to boost therapeutic efficacy. This paper reviews the recent advancements in understanding GLP-2, including its physiological roles and structure–activity relationships, and evaluates the development prospects of GLP-2 analogs.</div></div>","PeriodicalId":8806,"journal":{"name":"Biochemical pharmacology","volume":"233 ","pages":"Article 116758"},"PeriodicalIF":5.6000,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biochemical pharmacology","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0006295225000206","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/1/20 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
Glucagon-like peptide 2 (GLP-2) is a proglucagon-derived peptide released by intestinal endocrine cells. However, its therapeutic potential is limited by rapid inactivation via dipeptidyl peptidase-IV. The elucidation of three-dimensional structures of G-protein-coupled receptors, including GLP-2 receptor, has facilitated the rational design of novel peptide therapeutics. Recent studies have explored various structural modifications based on the structure of GLP-2, such as amino acid substitution, lipidation, and fusion with proteins, to extend the half-life of GLP-2 and enhance its biological activity. One promising avenue involves the development of multifunctional molecules targeting multiple pharmacological systems to boost therapeutic efficacy. This paper reviews the recent advancements in understanding GLP-2, including its physiological roles and structure–activity relationships, and evaluates the development prospects of GLP-2 analogs.
期刊介绍：
Biochemical Pharmacology publishes original research findings, Commentaries and review articles related to the elucidation of cellular and tissue function(s) at the biochemical and molecular levels, the modification of cellular phenotype(s) by genetic, transcriptional/translational or drug/compound-induced modifications, as well as the pharmacodynamics and pharmacokinetics of xenobiotics and drugs, the latter including both small molecules and biologics.
The journal''s target audience includes scientists engaged in the identification and study of the mechanisms of action of xenobiotics, biologics and drugs and in the drug discovery and development process.
All areas of cellular biology and cellular, tissue/organ and whole animal pharmacology fall within the scope of the journal. Drug classes covered include anti-infectives, anti-inflammatory agents, chemotherapeutics, cardiovascular, endocrinological, immunological, metabolic, neurological and psychiatric drugs, as well as research on drug metabolism and kinetics. While medicinal chemistry is a topic of complimentary interest, manuscripts in this area must contain sufficient biological data to characterize pharmacologically the compounds reported. Submissions describing work focused predominately on chemical synthesis and molecular modeling will not be considered for review.
While particular emphasis is placed on reporting the results of molecular and biochemical studies, research involving the use of tissue and animal models of human pathophysiology and toxicology is of interest to the extent that it helps define drug mechanisms of action, safety and efficacy.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
