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血管活性肠肽片段VIP(10 - 28)是结肠癌细胞系HT29中血管活性肠肽的拮抗剂。

A fragment of vasoactive intestinal peptide, VIP(10-28), is an antagonist of VIP in the colon carcinoma cell line, HT29.

作者信息

Turner J T, Jones S B, Bylund D B

出版信息

Peptides. 1986 Sep-Oct;7(5):849-54. doi: 10.1016/0196-9781(86)90105-1.

DOI:10.1016/0196-9781(86)90105-1
PMID:3025826
Abstract

The 19 amino acid carboxyl terminus fragment of vasoactive intestinal peptide (VIP), VIP(10-28), inhibits [125I]VIP binding in intact HT29 colonic adenocarcinoma cells and in membranes from these cells. However, VIP(10-28) alone has no effect on adenylate cyclase activity (membranes) or cyclic AMP synthesis (intact cells) in HT29 cells although VIP receptor agonists are markedly stimulatory. The indicated antagonist character of VIP(10-28) was confirmed by rightward parallel shifts of VIP dose response curves in the presence of VIP(10-28) in adenylate cyclase and cyclic AMP synthesis experiments. The equilibrium dissociation constant values for VIP(10-28) from these experiments agree with values from inhibition binding studies. The lack of effect of VIP(10-28) on forskolin dose response curves in HT29 adenylate cyclase assays indicates the specificity of the VIP(10-28) antagonism, thus suggesting that VIP(10-28) may be a useful tool in studying VIP receptor regulation and other aspects of the mechanisms of VIP action. The potential regulatory role of a proteolytically generated fragment of VIP acting antagonistically at VIP receptors is discussed.

摘要

血管活性肠肽（VIP）的19个氨基酸羧基末端片段VIP(10 - 28)，可抑制完整的HT29结肠腺癌细胞及其细胞膜中[125I]VIP的结合。然而，尽管VIP受体激动剂具有明显的刺激作用，但单独的VIP(10 - 28)对HT29细胞中的腺苷酸环化酶活性（细胞膜）或环磷酸腺苷合成（完整细胞）没有影响。在腺苷酸环化酶和环磷酸腺苷合成实验中，VIP(10 - 28)存在时VIP剂量反应曲线向右平行移动，证实了VIP(10 - 28)所示的拮抗剂特性。这些实验中VIP(10 - 28)的平衡解离常数值与抑制结合研究的值一致。在HT29腺苷酸环化酶测定中，VIP(10 - 28)对福斯可林剂量反应曲线无影响，表明了VIP(10 - 28)拮抗作用的特异性，因此提示VIP(10 - 28)可能是研究VIP受体调节及VIP作用机制其他方面的有用工具。本文还讨论了VIP经蛋白水解产生的片段在VIP受体上发挥拮抗作用的潜在调节作用。

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