β-内啡肽：8位和31位修饰类似物的合成与性质

beta-Endorphin: synthesis and properties of analogs modified in positions 8 and 31.

作者信息

Yamashiro D, Nicolas P, Li C H

出版信息

Int J Pept Protein Res. 1982 Jul;20(1):43-6. doi: 10.1111/j.1399-3011.1982.tb02650.x.

DOI:10.1111/j.1399-3011.1982.tb02650.x

Abstract

Four analogs of human beta-endorphin (beta h-EP) were synthesized by the solid-phase method: [Gln8,31]-beta h-EP(I), [Arg8,Gln31]-beta h-EP(II), [Ala8,Gln31]-beta h-EP (III), and [Val8, Gln31]-beta h-EP(IV). Radioreceptor binding assay with use of tritiated beta h-EP as primary ligand gave relative potencies as follows: beta h-EP, 100; I, 200;II, 150;III, 150;IV, 120. Relative potencies in an analgesic assay were: beta h-EP, 100; I,236;II, 254;III, 116;IV, 121. The side-chain of Glu-8 in beta h-EP can be replaced by a variety of structures without diminishing biological activity.

摘要

采用固相法合成了四种人β-内啡肽（βh-EP）类似物：[谷氨酰胺8,31]-βh-EP（I）、[精氨酸8,谷氨酰胺31]-βh-EP（II）、[丙氨酸8,谷氨酰胺31]-βh-EP（III）和[缬氨酸8,谷氨酰胺31]-βh-EP（IV）。以氚标记的βh-EP作为主要配体进行放射受体结合试验，得到的相对效价如下：βh-EP为100；I为200；II为150；III为150；IV为120。镇痛试验中的相对效价为：βh-EP为100；I为236；II为254；III为116；IV为121。βh-EP中谷氨酸-8的侧链可以被多种结构取代而不降低生物活性。