文献类型：期刊文献

英文题名：Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide-Target Interactions

作者：Shi, Yuxin[1,2];Chen, Yi[3];Deng, Liping[1];Du, Kui[1];Lu, Shaoyong[2,4,5];Chen, Ting[6]

机构：[1]Shaoxing Univ, Sch Chem & Chem Engn, Shaoxing 312000, Peoples R China;[2]Shanghai Jiao Tong Univ, Dept Pathophysiol, Key Lab Cell Differentiat & Apoptosis Chinese, Minist Educ, Shanghai 200025, Peoples R China;[3]Navy Med Univ, Eastern Hepatobiliary Surg Hosp, Dept Ultrasound Intervent, Shanghai 200433, Peoples R China;[4]Tongji Univ, Shanghai Peoples Hosp 10, Inst Energy Metab & Hlth, Sch Med, Shanghai 200072, Peoples R China;[5]Ningxia Med Univ, Coll Pharm, Yinchuan 750004, Ningxia Hui Aut, Peoples R China;[6]Naval Med Univ, Changzheng Hosp, Dept Cardiol, Shanghai 200003, Peoples R China

年份：0

外文期刊名：JOURNAL OF MEDICINAL CHEMISTRY

收录：SCI-EXPANDED(收录号：WOS:000914493000001)、、Scopus(收录号：2-s2.0-85146287487)、WOS

基金：ACKNOWLEDGMENTS This study was supported by grants from the National Natural Science Foundation of China (no. 22077082) , the Shanghai Frontiers Science Center of Cellular Homeostasis and the Human Diseases, and the Innovative Research Team of High-Level Local Universities in Shanghai.

语种：英文

外文摘要：The activation of G protein-coupled receptors (GPCRs) is triggered by ligand binding to their orthosteric sites, which induces ligand-specific conformational changes. Agonists and antagonists bound to GPCR orthosteric sites provide detailed information on ligand-binding modes. Among these, peptide ligands play an instrumental role in GPCR pharmacology and have attracted increased attention as therapeutic drugs. The recent breakthrough in GPCR structural biology has resulted in the remarkable availability of peptide-bound GPCR complexes. Despite the several structural similarities shared by these receptors, they exhibit distinct features in terms of peptide recognition and receptor activation. From this perspective, we have summarized the current status of peptide-bound GPCR structural complexes, largely focusing on the interactions between the receptor and its peptide ligand at the orthosteric site. In-depth structural investigations have yielded valuable insights into the molecular mechanisms underlying peptide recognition. This study would contribute to the discovery of GPCR peptide drugs with improved therapeutic effects.