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血管活性肠肽与人及大鼠肠膜中特定受体相互作用的结构要求：九个部分序列的影响

Structural requirements for VIP interaction with specific receptors in human and rat intestinal membranes: effect of nine partial sequences.

作者信息

Couvineau A, Rouyer-Fessard C, Fournier A, St Pierre S, Pipkorn R, Laburthe M

出版信息

Biochem Biophys Res Commun. 1984 Jun 15;121(2):493-8. doi: 10.1016/0006-291x(84)90209-2.

DOI:10.1016/0006-291x(84)90209-2
PMID:6329205
Abstract

Nine VIP sequences have been tested for their ability to inhibit the specific binding of 125I-VIP and to stimulate adenylate cyclase activity in intestinal epithelial membranes from rat and man. They are VIP 2-28; VIP 1-14; VIP 2-14; VIP 14-28; VIP 15-28; VIP 20-28; VIP 21-28 and two sequences where the N-terminal VIP 1-6 or VIP 1-9 have been joined covalently with the C-terminal VIP 20-28 or VIP 21-28. It appears that only VIP 2-28, VIP 14-28 and VIP 15-18 are able to inhibit competitively the binding of 125I-VIP to human and rat membranes. These analogues are respectively 88, 8,300 and 25,000 times less potent than VIP 1-28 in rat; they are respectively 70, 7,900 and 13,000 times less potent than VIP 1-28 in man. With respect to adenylate cyclase activation, VIP 14-28 and VIP 15-28 are very weak stimulators in the membranes from both species. VIP 2-28 behaves as a full VIP agonist in man whereas it is a partial VIP agonist in rat. These results indicate the structural importance of the whole VIP sequence for interacting with human and rat VIP receptors and further argue for a different structural requirement of rat and human receptors.

摘要

已对九条血管活性肠肽（VIP）序列抑制125I - VIP特异性结合以及刺激大鼠和人肠上皮细胞膜中腺苷酸环化酶活性的能力进行了测试。它们是VIP 2 - 28；VIP 1 - 14；VIP 2 - 14；VIP 14 - 28；VIP 15 - 28；VIP 20 - 28；VIP 21 - 28以及两条N端的VIP 1 - 6或VIP 1 - 9与C端的VIP 20 - 28或VIP 21 - 28共价连接的序列。似乎只有VIP 2 - 28、VIP 14 - 28和VIP 15 - 18能够竞争性抑制125I - VIP与人及大鼠细胞膜的结合。在大鼠中，这些类似物的效力分别比VIP 1 - 28低88倍、8300倍和25000倍；在人中，它们的效力分别比VIP 1 - 28低70倍、7900倍和13000倍。关于腺苷酸环化酶的激活，VIP 14 - 28和VIP 15 - 28在两种物种的膜中都是非常弱的刺激剂。VIP 2 - 28在人中表现为完全的VIP激动剂，而在大鼠中则是部分VIP激动剂。这些结果表明整个VIP序列对于与人及大鼠VIP受体相互作用的结构重要性，并进一步证明大鼠和人受体的结构要求不同。

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Structural requirements for VIP interaction with specific receptors in human and rat intestinal membranes: effect of nine partial sequences.血管活性肠肽与人及大鼠肠膜中特定受体相互作用的结构要求：九个部分序列的影响
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引用本文的文献

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