甘丙肽与大鼠胰腺β细胞及脑组织受体相互作用的结构要求

Structural requirements for galanin interaction with receptors from pancreatic beta cells and from brain tissue of the rat.

作者信息

Lagny-Pourmir I, Lorinet A M, Yanaihara N, Laburthe M

机构信息

INSERM U178, Unité de Recherches sur la Différenciation et la Neuroendocrinologie de Cellules Digestives, Bâtiment INSERM, Villejuif, France.

出版信息

Peptides. 1989 Jul-Aug;10(4):757-61. doi: 10.1016/0196-9781(89)90109-5.

DOI:10.1016/0196-9781(89)90109-5

PMID:2479930

Abstract

The binding activity of several galanin fragments and analogs was measured on specific receptors present in rat brain and the rat pancreatic beta cell line Rin m 5F. In both tissues it was observed that: 1) galanin(3-29), galanin(10-29) and [Ile2]-galanin were ineffective for inhibiting [125I] galanin binding and 2) active peptides had the following rank order of potency: galanin(1-29) greater than [Ac-Trp2]-galanin(2-29) greater than galanin(2-29) greater than galanin(1-15) greater than [Phe2]-galanin greater than [Tyr2]-galanin. It was concluded that the N-terminal portion of galanin is very important for interaction with central or peripheral receptors. The aromatic amino acid in position 2 (Trp in native galanin) plays a crucial role.

摘要

测定了几种甘丙肽片段和类似物对大鼠脑及大鼠胰腺β细胞系Rin m 5F中存在的特异性受体的结合活性。在这两种组织中均观察到：1）甘丙肽（3 - 29）、甘丙肽（10 - 29）和[异亮氨酸2] - 甘丙肽对抑制[125I]甘丙肽结合无效；2）活性肽的效价顺序如下：甘丙肽（1 - 29）＞[乙酰色氨酸2] - 甘丙肽（2 - 29）＞甘丙肽（2 - 29）＞甘丙肽（1 - 15）＞[苯丙氨酸2] - 甘丙肽＞[酪氨酸2] - 甘丙肽。得出的结论是，甘丙肽的N端部分对于与中枢或外周受体的相互作用非常重要。第2位的芳香族氨基酸（天然甘丙肽中的色氨酸）起关键作用。