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Molecular glues as GPCR modulators: unveiling three distinct mechanistic pathways for signal regulation

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资源类型：
Pubmed体系：
作者：
Xing Yuxuan[1,2] * ; Ao Jianyang[3,4] * ; Zhu Xiaoli[5] * ; Chai Zhengjun[6] ; Lu Shaoyong[1,2] ;
机构： [1]Shanghai Key Laboratory of Flexible Medical Robotics, Institute of Medical Robotics, Artificial Intelligence Clinical Research Center for Drug Discovery, Department of Pharmaceutical and Artificial-Intelligence Sciences, Tongren Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200336, China [2]Key Laboratory of Protection, Development and Utilization of Medicinal Resources in Liupanshan Area, Ministry of Education, Peptide & Protein Drug Research Center, School of Pharmacy, Ningxia Medical University, Yinchuan 750004, China [3]Department of Hepatobiliary and Pancreatic Surgery, Shanghai East Hospital, Tongji University School of Medicine, Shanghai 200120, China [4]Institute of Hepatobiliary and Pancreatic Surgery, Shanghai East Hospital, Tongji University School of Medicine, Shanghai 200120, China [5]Department of Emergency, The Third Affiliated Hospital of Naval Medical University, Shanghai 200438, China [6]Department of Thoracic, Shanghai East Hospital, School of Medicine, Tongji University, Shanghai 200120, China
出处：
DOI： 10.1016/j.drudis.2025.104484
ISSN：

关键词： G protein-coupled receptors (GPCRs) Molecular glues Intracellular allosteric site Biased signaling

摘要：
G protein-coupled receptors (GPCRs) constitute a large and pharmaceutically significant family of membrane proteins that mediate a wide range of physiological responses. Conventional modulation strategies primarily target orthosteric sites, but recent studies have identified a novel class of modulators known as 'molecular glues' that stabilize specific receptor-transducer interfaces. This review categorizes molecular glues into three mechanistic groups on the basis of their mode of action: those that directly stabilize receptor-transducer complexes, those that induce biased signaling through allosteric interactions, and those that modulate signaling indirectly by targeting allosteric regulatory sites. With advances in structural biology and computational methodologies, molecular glues are increasingly recognized as promising biased agonists, next-generation therapeutic agents, and valuable chemical tools for elucidating GPCR signaling pathways.Copyright © 2025 Elsevier Ltd. All rights reserved.

基金：
the National Key Research and Development Program of China (No. 2023YFC3404700) and the Noncommunicable Chronic Diseases-National Science and Technology Major Project fund (No. 2024ZD0531200).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2025]版：
大类 | 2 区 医学
小类 | 2 区 药学
最新[2025]版：
大类 | 2 区 医学
小类 | 2 区 药学
第一作者：
第一作者机构： [1]Shanghai Key Laboratory of Flexible Medical Robotics, Institute of Medical Robotics, Artificial Intelligence Clinical Research Center for Drug Discovery, Department of Pharmaceutical and Artificial-Intelligence Sciences, Tongren Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200336, China [2]Key Laboratory of Protection, Development and Utilization of Medicinal Resources in Liupanshan Area, Ministry of Education, Peptide & Protein Drug Research Center, School of Pharmacy, Ningxia Medical University, Yinchuan 750004, China
共同第一作者：
通讯作者：
通讯机构： [1]Shanghai Key Laboratory of Flexible Medical Robotics, Institute of Medical Robotics, Artificial Intelligence Clinical Research Center for Drug Discovery, Department of Pharmaceutical and Artificial-Intelligence Sciences, Tongren Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200336, China [2]Key Laboratory of Protection, Development and Utilization of Medicinal Resources in Liupanshan Area, Ministry of Education, Peptide & Protein Drug Research Center, School of Pharmacy, Ningxia Medical University, Yinchuan 750004, China
推荐引用方式(GB/T 7714)：
Xing Yuxuan,Ao Jianyang,Zhu Xiaoli,et al.Molecular glues as GPCR modulators: unveiling three distinct mechanistic pathways for signal regulation[J].Drug Discovery Today.2025,104484.doi:10.1016/j.drudis.2025.104484.
APA：
Xing Yuxuan,Ao Jianyang,Zhu Xiaoli,Chai Zhengjun&Lu Shaoyong.(2025).Molecular glues as GPCR modulators: unveiling three distinct mechanistic pathways for signal regulation.Drug Discovery Today,,
MLA：
Xing Yuxuan,et al."Molecular glues as GPCR modulators: unveiling three distinct mechanistic pathways for signal regulation".Drug Discovery Today .(2025):104484

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