Conformational Dynamics of Large 'Two-Headed Ligand Keys': Unlocking the Glucagon-Like Peptide-1 Receptor Signaling Pathway

机译：大“双头配体键”的构象动态：解锁胰高血糖素样肽-1受体信号传导路径

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The glucagon-like peptide-1 receptor (GLP-1R) potentiates glucose-stimulated insulin secretion and is a therapeutic target for treat ment of type 2 diabetes mellitus. Like other class-B G-protein-coupled receptors (GPCRs), GLP-1R possesses a large extracellular domain (145 residues) which binds to the carboxyl-terminal regions of peptide ligands. This allows the trans-membrane region to interact with the amino-terminal portion of the peptide ligands which induces a structural rearrangement in the receptor that potentiates intracellular G-pr otein signaling. Hydrogen/Deut erium Exchange (HDX) with Electron Transfer Dissociation (ETD) has been used to characterize GLP-1R signaling and develop a platform to screen novel therapeutics for type II diabetes.

机译：胰高血糖素样肽-1受体（GLP-1R）增强葡萄糖刺激的胰岛素分泌，是治疗2型糖尿病的治疗靶标。与其他类-B G蛋白偶联受体（GPCR）相同，GLP-1R具有大的细胞外结构域（145个残基），其与肽配体的羧基末端区域结合。这允许跨膜区域与肽配体的氨基 - 末端部分相互作用，该配体诱导受体中具有增强细胞内G-PR OTEIN信号传导的受体中的结构重排。具有电子转移解离（ETD）的氢气/乙酰·乙酸伊硫交换（HDX）已用于表征GLP-1R信号传导，并开发平台，以筛选II型糖尿病的新型治疗剂。

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《American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics》|2012年||共2页
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Graham M. West; Kyle W. Sloop; Francis S. Willard; Michael C. Chalmers; Bruce D. Pascal; Jeffery A. Dodge; Patrick R. Griffin;
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1. Glucagon-like peptide-1 receptor is present on human hepatocytes and has a direct role in decreasing hepatic steatosis in vitro by modulating elements of the insulin signaling pathway. [J] . Gupta NA, Mells J, Dunham RM, Hepatology: Official Journal of the American Association for the Study of Liver Diseases . 2010,第5期

机译：胰高血糖素样肽-1受体存在于人肝细胞上，并通过调节胰岛素信号传导途径的元素在体外减少肝脂肪变性中具有直接作用。
2. The food intake-suppressive effects of glucagon-like peptide-1 receptor signaling in the ventral tegmental area are mediated by AMPA/kainate receptors [J] . Mietlicki-BaaseE.G., OrtinskiP.I., RupprechtL.E., American Journal of Physiology . 2013,第6aPta1期

机译：胰高血糖素样肽-1受体信号传导在腹侧被盖区的食物摄取抑制作用由AMPA /海藻酸酯受体介导
3. A model for receptor-peptide binding at the glucagon-like peptide-1 (GLP-1) receptor through the analysis of truncated ligands and receptors. [J] . Al Sabah S, Donnelly D British Journal of Pharmacology . 2003,第2期

机译：通过分析截短的配体和受体，在胰高血糖素样肽-1（GLP-1）受体上结合受体-肽的模型。
4. Conformational Dynamics of Large "Two-Headed Ligand Keys": Unlocking the Glucagon-Like Peptide-1 Receptor Signaling Pathway [C] . Graham M. West, Kyle W. Sloop, Francis S. Willard, American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics . 2012

机译：大“双头配体键”的构象动态：解锁胰高血糖素样肽-1受体信号传导路径
5. Combinatorial targeting of the glucagon-like peptide-1 and sulfonylurea-1 receptors using a complimentary mulitvalent glucagon-like peptide-1/glibenclamide ligand for the improvement of beta-cell targeting agents and diabetic treatment. [D] . Hart, Nathaniel. 2013

机译：使用互补的多价胰高血糖素样肽-1 /格列苯脲酰胺配体对胰高血糖素样肽-1和磺酰脲-1受体进行联合靶向，以改善β细胞靶向剂和糖尿病治疗。
6. Cell Signaling: Proteins Pathways and Mechanisms: Modeling analysis of inositol 145-trisphosphate receptor-mediated Ca2+ mobilization under the control of glucagon-like peptide-1 in mouse pancreatic β-cells [O] . Yukari Takeda, Takao Shimayoshi, George G. Holz, -1

机译：细胞信号转导：蛋白质途径和机制：小鼠胰岛β细胞中胰高血糖素样肽1控制下肌醇145-三磷酸受体介导的Ca2 +动员的建模分析
7. Glucagon-Like Peptide-1 Receptor Mediates the Improvement of Glycolipid Metabolism Disorder via AKT and AMPK Signaling Pathways in L02 with Insulin Resistance [O] . Qiao ji Tian, Yifeng Liu, Peng Yuan, 2020

机译：胰高血糖素类肽-1受体通过L02中的AKT和AMPK信号传导途径介导糖脂代谢障碍的改善，具有胰岛素抵抗力

Conformational Dynamics of Large 'Two-Headed Ligand Keys': Unlocking the Glucagon-Like Peptide-1 Receptor Signaling Pathway

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