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Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine

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收录情况： ◇ SCIE ◇ 自然指数

作者：
Zhao Jie[1] * ; Fu Hong[1] * ; Yu Jingjing[1] * ; Hong Weiqi[1] * ; Tian Xiaowen[1] * ; Qi Jieyu[2] * ; Sun Suyue[1] ; Zhao Chang[1] ; Wu Chao[1] ; Xu Zheng[1] ; Cheng Lin[3] ; Chai Renjie[2,3,4] ; Yan Wei[1] ; Wei Xiawei[1] ; Shao Zhenhua[1,5] ;
机构： [1]Division of Nephrology and Kidney Research Institute, Laboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics,West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China. [2]State Key Laboratory of Bioelectronics, Department of Otolaryngology Head and Neck Surgery, Zhongda Hospital, School of Life Sciences and Technology, Advanced Institute for Life and Health, Jiangsu Province High-Tech Key Laboratory for Bio-Medical Research, Southeast University, Nanjing 210096, China. [3]Department of Otolaryngology Head and Neck Surgery, Sichuan Provincial People’s Hospital, University of Electronic Science and Technology of China, Chengdu, China. [4]Co-Innovation Center of Neuroregeneration, Nantong University, Nantong 226001, China. [5]Department of Nephrology, Hainan General Hospital, Haikou, Hainan 570311, China.
出处：
DOI： 10.1038/s41467-023-36673-z
ISSN：

摘要：
Somatostatin receptor 2 (SSTR2) is highly expressed in neuroendocrine tumors and represents as a therapeutic target. Several peptide analogs mimicking the endogenous ligand somatostatin are available for clinical use, but poor therapeutic effects occur in a subset of patients, which may be correlated with subtype selectivity or cell surface expression. Here, we clarify the signal bias profiles of the first-generation peptide drug octreotide and a new-generation small molecule paltusotine by evaluating their pharmacological characteristics. We then perform cryo-electron microscopy analysis of SSTR2-Gi complexes to determine how the drugs activate SSTR2 in a selective manner. In this work, we decipher the mechanism of ligand recognition, subtype selectivity and signal bias property of SSTR2 sensing octreotide and paltusotine, which may aid in designing therapeutic drugs with specific pharmacological profiles against neuroendocrine tumors.© 2023. The Author(s).

基金：
This researchwas supported by theNationalNatural Science Foundation ofChina (32100988 toW.Y.; 32200986 to J.Z.; 31972916 to Z.S.), Science and Technology Department of Sichuan Province (2021ZYD0080 to W.Y.), National Key R&D Program of China (2019YFA0508800 to Z.S.), the National Science Foundation for Excellent Young Scholars (32122052 to X.W.), National Natural Science Foundation Regional Innovation and Development (No. U19A2003 to X.W.), the China Postdoctoral Science Foundation (BX20220219 to Z.X.; 2022M712275 to J.Z.) and Post-Doctor Research Project, West China Hospital, Sichuan University (2021HXBH064 to J.Z.).
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外文
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中科院(CAS)分区：
出版当年[2023]版：
大类 | 1 区 综合性期刊
小类 | 1 区 综合性期刊
最新[2023]版：
大类 | 1 区 综合性期刊
小类 | 1 区 综合性期刊
JCR分区：
出版当年[2023]版：
Q1 MULTIDISCIPLINARY SCIENCES
最新[2023]版：
Q1 MULTIDISCIPLINARY SCIENCES

影响因子： 最新[2023版] 最新五年平均 出版当年[2023版] 出版当年五年平均 出版前一年[2022版]

第一作者：
第一作者机构： [1]Division of Nephrology and Kidney Research Institute, Laboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics,West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.
共同第一作者：
通讯作者：
通讯机构： [1]Division of Nephrology and Kidney Research Institute, Laboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics,West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China. [2]State Key Laboratory of Bioelectronics, Department of Otolaryngology Head and Neck Surgery, Zhongda Hospital, School of Life Sciences and Technology, Advanced Institute for Life and Health, Jiangsu Province High-Tech Key Laboratory for Bio-Medical Research, Southeast University, Nanjing 210096, China. [3]Department of Otolaryngology Head and Neck Surgery, Sichuan Provincial People’s Hospital, University of Electronic Science and Technology of China, Chengdu, China. [4]Co-Innovation Center of Neuroregeneration, Nantong University, Nantong 226001, China. [5]Department of Nephrology, Hainan General Hospital, Haikou, Hainan 570311, China.
推荐引用方式(GB/T 7714)：
Zhao Jie,Fu Hong,Yu Jingjing,et al.Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine[J].NATURE COMMUNICATIONS.2023,14(1):doi:10.1038/s41467-023-36673-z.
APA：
Zhao Jie,Fu Hong,Yu Jingjing,Hong Weiqi,Tian Xiaowen...&Shao Zhenhua.(2023).Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine.NATURE COMMUNICATIONS,14,(1)
MLA：
Zhao Jie,et al."Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine".NATURE COMMUNICATIONS 14..1(2023)

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