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中国生物化学与分子生物学会第十二届全国会员代表大会暨2018年全国学术会议

作者： Beili Wu CAS Key Laboratory of receptor Research Shanghai Institute of Materia MedicaChinese Academy of Sciences

The human glucagon receptor(GCGR) belongs to the class B G protein-coupled receptor(GPCR) family and plays a key role in glucose homeostasis and the pathophysiology of type 2 *** we report two crystal structures of full-length GCGR containing both extracellular domain(ECD) and transmembrane domain(TMD) at different conformational ***,the stalk region,which connects the ECD and TMD,and the first extracellular loop(ECL1) undergo major conformational changes in secondary structure during peptide ligand binding,forming key interactions with the ***/deuterium exchange,disulfide cross-linking and molecular dynamics studies suggest that the stalk and ECL1 play critical roles in modulating peptide ligand binding and receptor *** further propose a dual-binding-site trigger model for GCGR activation,which requires conformational changes of the stalk,ECL1 and *** insights into the full-length GCGR structure deepen our understanding about the signaling mechanisms of class B GPCRs.

关键词： GPCR glucagon receptor signaling structural studies

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In vitro selection and identifcation of DNA aptamer against glucagon receptor by cell-SELEX

In vitro selection and identifcation of DNA aptamer against ...

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华东地区生物化学与分子生物学学会联合会2017年学术交流会暨安徽省生物化学与分子生物学学会理事会议

作者： Guodong Wang Jun Liu Yiling Xu Lei Zhu Xiaoxiao Hu Jianglin Li Wen Zhong Huixia Liu Weihong Tan Anhui Provincial Engineering Research Center for Polysaccharide Drugs School of PharmacyWannan Medical College Xiangya Hospital Central South University Molecular Science and Biomedicine Laboratory State Key Laboratory for Chemo/Bio-Sensing and ChemometricsCollege of Chemistry and Chemical EngineeringCollege of BiologyHunan University

glucagon,a functional insulin antagonist,is a pivotal counter-regulatory hormone in the regulation of glucose *** secretion of glucagon significantly contributes to *** exerts its physiological functions through activation of the glucagon receptor(GCGR).Inhibition of GCGR activity represents a potential therapeutic approach for reducing excess glucose production in diabetes *** efforts have been undertaken by the pharmaceutical industry to develop potent small molecule glucagon receptor antagonists or antibodies for clinical *** glucagon receptor antagonists and antibodies able to improve glucose homeostasis in animal models and humans have been ***,thus far none has progressed to final marketing approval,mainly due to a poor performance profile,including toxicity or lack of *** are short DNA or RNA oligonucleotides evolved from systematic evolution of ligands by exponential enrichment(SELEX).They can act as ligands with specific and high binding affinity for a variety of targets,including small molecules,proteins,nucleic acids,viruses,bacteria,cells and *** molecular recognition properties of aptamers are similar to those of ***,manmade aptamers possess several advantages over naturally occurring antibodies,including economical and reproducible synthesis,easy modification,low toxicity,high stability,lack of immunogenicity,and rapid tissue *** addition to recognition,some aptamers are able to retain their function to regulate biological pathways and interfere with disease development through binding to molecular targets involved in *** on these advantages,aptamers show high potential for therapeutic applications,such as targeted therapy,detection and *** this study,we have successfully selected a DNA aptamer against GCGR by cell-SELEX after 16 rounds of evolved *** selected aptamer,GR-3,can specifically bi

关键词： glucagon receptor aptamer cell-SELEX diabetes mellitus binding affinity

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Highly efficient detection of insulinotropic action of glucagon via GLP-1 receptor in mice pancreatic beta-cell with a novel perfusion microchip

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Chinese Chemical Letters 2016年第7期27卷 1027-1031页

作者： Li-Dan Hu Yu-Lin Zhang Hong Wang Xing-Yue Peng Yi Wang School of Life Sciences. Xiamen University. Xiamen 361005. China Laboratory of Cardiometabolic Molecular Medicine Institute of Molecular Medicine Peking University Beijing 100871 China College of Life Sciences and Technology Huazhong University of Science and Technology Wuhan 430074 China

glucagon exhibits insulinotropic ability by activating cAMP through glucagon or glucagon-like peptide-1（GLP-1） *** investigate the mechanism of endogenous and exogenous glucagon on insulin release,we studied the receptor selectivity on pancreatic islet beta-cells by switching the glucose concentration from 20 mmol/L to 0 mmol/L To measure the exact temporal relationship between glucagon and insulin release,we developed a quick,small volume,multi-channel polydimethylsiloxane（PDMS） *** 0 mmol/L glucose,we observed an insulinotropic effect in both INS-1 cells and ***,we observed a 63 ± 6.27 s delay of endogenous glucagon-induced insulin *** treatment with glucagon and GLP-1 receptor antagonists,we found that endogenous glucagon utilized the glucagon receptor,whereas exogenous glucagon primarily utilized the GLP-1 receptor to promote insulin *** microchip can also be used to describe the ＂glucagonocentric＂ vision of diabetes *** together,the insulinotropic mechanism of different receptors should be taken into account in clinical treatments.

关键词： glucagon Insulin glucagon receptor GLP-1 receptor Microchip

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Design and discovery of a highly potent ultralong-acting GLP-1 and glucagon co-agonist for attenuating renal fibrosis

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Acta Pharmaceutica Sinica B 2024年第3期14卷 1283-1301页

作者： Qian Zhao Jiale Dong Han Liu Hui Chen Huan Yu Shuyin Ye Shuangjin Yu Yu Li Longhui Qiu Nazi Song Hongjiao Xu Qi Liu Zhiteng Luo Yuyi Li Rui Wang Guodong Chen Xianxing Jiang School of Pharmaceutical Sciences Guangdong Provincial Key Laboratory of Chiral Molecule and Drug DiscoverySun Yat-sen UniversityGuangzhou 510006China Organ Transplant Center the First Affiliated HospitalSun Yat-sen UniversityGuangzhou 510006China Zhongshan School of Medicine Sun Yat-sen UniversityGuangzhou 510006China Shenzhen Turier Biotech.Co. Ltd.Shenzhen 518118China School of Life Sciences Key Laboratory of Preclinical Study for New Drugs of Gansu ProvinceSchool of Basic Medical Sciences&Research Unit of Peptide ScienceChinese Academy of Medical SciencesLanzhou UniversityLanzhou 730000China

The role of co-agonists of glucagon-like peptide-1 receptor(GLP-1R)and glucagon receptor(GCGR)in chronic kidney disease(CKD)remains *** we found that GLP-1R and GCGR expression levels were lower in the kidneys of mice with CKD compared to healthy mice and were correlated with disease ***,GLP-1R or GCGR knockdown aggravated the progression of kidney injury in both diabetic db/db mice and non-diabetic mice undergoing unilateral ureteral obstruction(UUO).Based on the importance of GLP-1R and GCGR in CKD,we reported a novel monomeric peptide,1907-B,with dual-agonism on both GLP-1R and *** data confirmed that 1907-B had a longer half-life than long-acting semaglutide in rats or cynomolgus monkeys(~2-3 fold)and exhibited better therapeutic contribution to CKD than best-in-class monoagonists,semaglutide,or glucagon,in db/db mice and UUO *** lock-of-function models,including selective pharmacological activation and genetic knockdown,confirmed that 1907-B’s effects on ameliorating diabetic nephropathy in db/db mice,as well as inhibiting kidney fibrosis in UUO mice,were mediated through GLP-1 and glucagon *** findings highlight that 1907-B,a novel GLP-1R and GCGR co-agonist,exerts multifactorial improvement in kidney injuries and is an effective and promising therapeutic option for CKD treatment.

关键词： GLP-1 receptor glucagon receptor Chronic kidney disease Diabetic nephropathy Kidney fibrosis Dual-agonism

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Pathologic pancreatic endocrine cell hyperplasia

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World Journal of Gastroenterology 2011年第2期17卷 137-143页

作者： Debra Ouyang Deepti Dhall Run Yu Department of Medicine Cedars-Sinai Medi-cal Center Los Angeles CA 90048 United States Department of Pathology Cedars-Sinai MedicalCenter Los Angeles CA 90048 United States Division of Endocrinology and Carcinoid and Neu-roendocrine Tumor Center Cedars-Sinai Medical Center LosAngeles CA 90048 United States

Pathologic hyperplasia of various pancreatic endocrine cells is rare but has been long known.β cell hyperplasia contributes to persistent hyperinsulinemic hypoglycemia of infancy,which is commonly caused by mutations in the islet ATP-sensitive potassium channel,and to noninsulinoma pancreatogenous hypoglycemia in adults,which may or may not be associated with bariatric surgery.α cell hyperplasia may cause glucagonoma syndrome or induce pancreatic neuroendocrine *** inactivating mutation of the glucagon receptor causes α cell hyperplasia and asymptomatic *** polypeptide cell hyperplasia has been described without a clearly-characterized clinical syndrome and hyperplasia of other endocrine cells inside the pancreas has not been reported to our knowledge. Based on morphological evidence,the main pathogenetic mechanism for pancreatic endocrine cell hyperplasia is increased endocrine cell neogenesis from exocrine ductal *** endocrine cell hyperplasia should be considered in the diagnosis and management of hypoglycemia,elevated islet hormone levels,and pancreatic neuroendocrine *** studies of pathologic pancreatic endocrine cell hyperplasia will likely yield insights into the pathogenesis and treatment of diabetes and pancreatic neuroendocrine tumors.

关键词： glucagon receptor Hyperplasia Nesidioblastosis Islet Pancreatic endocrine cell Neuroendocrine tumor

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