Structures of the endogenous peptide-and selective non-peptide agonist-bound SSTR2 signaling complexes  

作　　者：Li-Nan Chen Wei-Wei Wang Ying-Jun Dong Dan-Dan Shen Jia Guo Xuefei Yu Jiao Qin Su-Yu Ji Huibing Zhang Qingya Shen Qiaojun He Bo Yang Yan Zhang Qinglin Li Chunyou Mao 

机构地区：[1]Department of Biophysics and Department of Pathology of Sir Run Run Shaw Hospital,Zhejiang University,School of Medicine,Hangzhou,Zhejiang,China [2]Department of General Surgery,Sir Run Run Shaw Hospital,Zhejiang University School of Medine,Hangzhou,Zhejiang,China [3]Center for Structural Pharmacology and Therapeutics Development,Sir Run Run Shaw Hospital,Zhejiang University School of Medicine,Hangzhou,Zhejiang,China [4]Liangzhu Laboratory,Zhejiang University Medical Center,Hangzhou,Zhejiang,China [5]The Cancer Hospital of the University of Chinese Academy of Sciences(Zhejiang Cancer Hospital),Hangzhou,Zhejiang,China [6]Zhejiang Province Key Laboratory of Anti-Cancer Drug Research,College of Pharmaceutical Sciences,Zhejiang University,Hangzhou,Zhejiang,China [7]MOE Frontier Science Center for Brain Research and Brain-Machine Integration,Zhejiang University School of Medicine,Hangzhou,Zhejiang,China [8]Zhejiang Provincial Key Laboratory of Immunity and Inflammatory diseases,Hangzhou,Zhejiang,China

出　　处：《Cell Research》2022年第8期785-788,共4页细胞研究（英文版）

基　　金：supported by the National Natural Science Foundation of China(81922071 to Y.Z.and 32100959 to C.M.);Zhejiang Province Natural Science Fund for Excellent Young Scholars(LR19H31000 to Y.Z.and LR22C050002 to C.M.);the Ministry of Science and Technology(2019YFA050880 to Y.Z.);the Key R&D Projects of Zhejiang Province(2021C03039 to Y.Z.).

摘　　要：Dear Editor,Somatostatin,also known as growth hormone-inhibiting hormone,is an important peptide hormone that mediates predominanty neuroendocrine inhibitory effects in the exocrine and endocrine systems,12 Besides,t can also exert potent regulatory effects on cell proliferation and angiogenesis.3 In human,somatostatin exerts its physiological functions through activating five somatostatin receptors(SSTRs),which are class A Gvo protein-coupled receptors,Pharmacologicaly,somatostatin receptors,especially SSTR2,are the primary drug targets for the treatment of pituitary adenomas and neuroendocrine tumors.-s To date,three somatostatin analogs have been approved for clinical use and two of them(lanreotide and octreotide)are sSTR2-selective drugs.3 In addition to peptidic agonists,extensive efforts have also been made to design selective small-molecule agonists,t which will failitate the development of orly active chemotherapeutic agents.

关 键 词：COMPLEXES ANALOGS predominant 

分 类 号：Q2[生物学—细胞生物学]