Differential engagement of polar networks in the glucagon-like peptide 1 receptor by endogenous variants of the glucagon-like peptide 1

S.G.B. Furness; A. Christopoulos; P.M. Sexton; D. Wootten

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Differential engagement of polar networks in the glucagon-like peptide 1 receptor by endogenous variants of the glucagon-like peptide 1

机译：极地网络在胰高血糖素样肽1受体中的差异啮合通过胰高血糖素样肽1的内源性变体

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摘要

The glucagon-like peptide 1 receptor (GLP-1R) can be activated by a number of endogenous peptide hormones, including extended, processed, glycine extended and carboxy-terminally amidated versions of glucagon-like peptide 1 (GLP-1). While the main focus of the literature has been on the processed, amidated form, GLP-1(7-36)NH2, the other forms of this peptide are likely to be secreted in physiologically relevant amounts under certain circumstances. This study builds on our existing work examining the effect of mutation of conserved transmembrane polar residues within the receptor to understand the nature of binding and pleiotropic signaling in response to these alternatively processed versions of this important incretin hormone. We show that extended and processed peptides differ not only in their binding to the receptor but also in the way the receptor is engaged for activation that leads to differential signaling bias exhibited by these peptides.

机译：胰高血糖素样肽1受体（GLP-1R）可以通过多种内源肽激素激活，包括延长，加工，甘氨酸延伸和羧基 - 末端酰胺化的胰高血糖素样肽1（GLP-1）。虽然文献的主要焦点一直在加工，酰胺化形式，GLP-1（7-36）NH 2，这种肽的其他形式可能在某些情况下在生理相关金额中分泌。本研究建立了我们现有的作品，检查了受体内保守跨膜极性残基突变的突变，了解响应于这些重要的Incetin激素的这些可选择加工版本的结合和抗血液发信号的性质。我们表明，延长和加工的肽不仅不同于与受体的结合而不同，而且在接受受体接合激活的方式导致这些肽表现出的差分信号传导偏差。

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来源
《Biochemical Pharmacology》 |2018年第2018期|共18页
作者
S.G.B. Furness; A. Christopoulos; P.M. Sexton; D. Wootten;
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作者单位

Drug Discovery Biology Monash Institute of Pharmaceutical Sciences and Department of Pharmacology;

Drug Discovery Biology Monash Institute of Pharmaceutical Sciences and Department of Pharmacology;

Drug Discovery Biology Monash Institute of Pharmaceutical Sciences and Department of Pharmacology;

Drug Discovery Biology Monash Institute of Pharmaceutical Sciences and Department of Pharmacology;

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原文格式 PDF
正文语种 eng
中图分类药理学;
关键词
Cell signaling; G protein coupled receptors (GPCRs); Receptor structure-function; Signal transduction; Glucagon-like peptide-1 receptor; Biased agonism;

机译：细胞信号;G蛋白偶联受体（GPCR）;受体结构功能;信号转导;胰高血糖素样肽-1受体;偏见激动;

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专利

1. Differential engagement of polar networks in the glucagon-like peptide 1 receptor by endogenous variants of the glucagon-like peptide 1 [J] . S.G.B. Furness, A. Christopoulos, P.M. Sexton, Biochemical Pharmacology . 2018,第期

机译：极地网络在胰高血糖素样肽1受体中的差异啮合通过胰高血糖素样肽1的内源性变体
2. The contribution of serotonin 5-HT2C and melanocortin-4 receptors to the satiety signaling of glucagon-like peptide 1 and liraglutide, a glucagon-like peptide 1 receptor agonist, in mice. [J] . Nonogaki K, Suzuki M, Sanuki M, Biochemical and Biophysical Research Communications . 2011,第2期

机译：5-羟色胺5-HT2C和黑皮质素-4受体对小鼠中胰高血糖素样肽1和利拉鲁肽（一种胰高血糖素样肽1受体激动剂）的饱腹感信号的贡献。
3. The contribution of serotonin 5-HT2C and melanocortin-4 receptors to the satiety signaling of glucagon-like peptide 1 and liraglutide, a glucagon-like peptide 1 receptor agonist, in mice. [J] . Nonogaki K, Suzuki M, Sanuki M, Biochemical and Biophysical Research Communications . 2011,第2期

机译：5-羟色胺5-HT2C和黑皮质素-4受体对小鼠中胰高血糖素样肽1和利拉鲁肽（一种胰高血糖素样肽1受体激动剂）的饱腹感信号的贡献。
4. HIGH-LEVEL EXPRESSION OF GLUCAGON AND GLUCAGON-LIKE PEPTIDE 1 RECEPTORS IN TETRACYCLINE-INDUCIBLE STABLE HEK293S GNTI-CELLS [C] . Cecilia G. Unson the European Peptide Symposium . 2007

机译：胰高血糖素和胰高血糖素样肽1受体在四环素 - 诱导稳定HEK293S GNTI细胞中的高水平表达
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. The major determinant of exendin-4/glucagon-like peptide 1 differential affinity at the rat glucagon-like peptide 1 receptor N-terminal domain is a hydrogen bond from SER-32 of exendin-4 [O] . RJ Mann, NE Nasr, JK Sinfield, 2010

机译：exendin-4 /胰高血糖素样肽1在大鼠胰高血糖素样肽1受体N端结构域的亲和力差异的主要决定因素是exendin-4 SER-32的氢键
7. Interactions of a Glucagon-like peptide 1 and a Glucagon-like peptide 1 analogue, liraglutide, with the endogenous receptor [O] . Frederiksen Tine Maja, Harris Pernille, Bukrinski Jens T., 2015

机译：胰高血糖素样肽1和胰高血糖素样肽1类似物利拉鲁肽与内源性受体的相互作用

Differential engagement of polar networks in the glucagon-like peptide 1 receptor by endogenous variants of the glucagon-like peptide 1

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