Structural requirements of the N-terminal region of GLP-1-(7-37)-NH(2) for receptor interaction and cAMP production.

Sarrauste De Menthiere C; Chavanieu A; Grassy G; Dalle S; Salazar G; Kervran A; Pfeiffer B; Renard P; Delagrange P; Manechez D; Bakes D; Ktorza A; Calas B

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Structural requirements of the N-terminal region of GLP-1-(7-37)-NH(2) for receptor interaction and cAMP production.

机译：GLP-1-（7-37）-NH（2）N末端区域的结构要求，用于受体相互作用和cAMP产生。

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A series of GLP-1-[7-36]-NH(2) (tGLP-1) and GLP-1-[7-37] analogs modified in position 7, 8, 9 and 36, have been designed and evaluated on murine GLP-1 receptors expressed in RIN T3 cells for both their affinity and activity. Ten of the synthesized peptides were found full agonists with activities superior or at least equal to that of the native hormone. Five of them were investigated for their plasmatic stability and the most stable, [a(8)-desR(36)]GLP-1-[7-37]- NH(2) (Compound 8), evaluated in vivo in a glucose tolerance test which confirmed a clearly longer activity than that of the native hormone. We also performed circular dichroism study and propose a hypothetical structural model explaining the most part of observed activities of GLP-1 analogs on RIN T3 cells.

机译：已设计并评估了在位置7、8、9和36上修饰的一系列GLP-1- [7-36] -NH（2）（tGLP-1）和GLP-1- [7-37]类似物。 RIN T3细胞中表达的鼠GLP-1受体具有亲和力和活性。发现十种合成的肽具有高于或至少等于天然激素的活性的完全激动剂。研究了其中五种化合物的血浆稳定性和最稳定的[a（8）-desR（36）] GLP-1- [7-37]-NH（2）（化合物8），在葡萄糖中进行了体内评估耐受性测试证实其活性明显长于天然激素。我们还进行了圆二色性研究，并提出了一种假设的结构模型，该模型解释了观察到的GLP-1类似物对RIN T3细胞的大部分活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2004年第6期|共8页
作者
Sarrauste De Menthiere C; Chavanieu A; Grassy G; Dalle S; Salazar G; Kervran A; Pfeiffer B; Renard P; Delagrange P; Manechez D; Bakes D; Ktorza A; Calas B;
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正文语种 eng
中图分类基础医学;
关键词
glucagon-like peptide 1; No history of; receptor; liothyronine sodium;

机译：胰高血糖素样肽1;无病史;受体;碘甲状腺素钠;

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1. Structural requirements of the N-terminal region of GLP-1-(7-37)-NH(2) for receptor interaction and cAMP production. [J] . Sarrauste De Menthiere C, Chavanieu A, Grassy G, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2004,第6期

机译：GLP-1-（7-37）-NH（2）N末端区域的结构要求，用于受体相互作用和cAMP产生。
2. H-1 NMR structural and functional characterisation of a cAMP-specific phosphodiesterase-4D5 (PDE4D5) N-terminal region peptide that disrupts PDE4D5 interaction with the signalling scaffold proteins, arrestin and RACK1 [J] . Smith KJ, Baillie GS, Hyde EI, Cellular Signalling . 2007,第12期

机译：H-1 NMR的cAMP特异性磷酸二酯酶4D5（PDE4D5）N端区域肽的结构和功能表征，可破坏PDE4D5与信号支架蛋白，抑制蛋白和RACK1的相互作用
3. Dynamic, inter-subunit interactions between the N-terminal and central mutation regions of cardiac ryanodine receptor. [J] . Liu Z, Wang R, Tian X, Journal of Cell Science . 2010,第10期

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4. NMR STRUCTURAL ANALYSIS OF THE HIV-1 GP120 V3 - CCR5 CO-RECEPTOR N-TERMINAL INTERACTION [C] . Petros A. Galanakis, Nikolaos Kandias, Georgios A. Spyroulias the European Peptide Symposium . 2007

机译：HIV-1 GP120 V3 - CCR5共受体N末端相互作用的NMR结构分析
5. The structural basis of chemokine binding affinity and receptor selectivity: Role of receptor N-terminal domain [D] . Ravindran, Aishwarya 2010

机译：趋化因子结合亲和力和受体选择性的结构基础：受体N末端结构域的作用
6. Dynamic inter-subunit interactions between the N-terminal and central mutation regions of cardiac ryanodine receptor [O] . Zheng Liu, Ruiwu Wang, Xixi Tian, -1

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Structural requirements of the N-terminal region of GLP-1-(7-37)-NH(2) for receptor interaction and cAMP production.

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