β-内啡肽。具有二硫键的类似物的合成与生物活性。
Beta-endorphin. Synthesis and biological activity of analogs with disulfide bridges.
作者信息
Blake J, Helmeste D M, Li C H
出版信息
Int J Pept Protein Res. 1985 Jun;25(6):575-9. doi: 10.1111/j.1399-3011.1985.tb02212.x.
Two analogs of human beta-endorphin (beta-EP) which contain cystine bridges, [Cys15-Cys26,Phe27,Gly31]-beta-EP (I) and [Cys16-Cys26,Phe27,Gly31]-beta-EP (II), were synthesized by the solid-phase method. Peptides I and II were shown to contain 2-2.5 times the opiate receptor binding activity of beta-endorphin. We also synthesized two analogs with reduced alkylated cysteine residues and these peptides, [Arg9,19,24,28,29 Cys(Cam)11,26,Phe27,Gly31] and [Arg9,19,24,28,29,Cys-(Cam)12,26,Phe27,Gly31], were shown to have approximately the same opiate receptor activity as beta-endorphin.
通过固相法合成了两种含有胱氨酸桥的人β-内啡肽（β-EP）类似物，即[Cys15-Cys26，Phe27，Gly31]-β-EP（I）和[Cys16-Cys26，Phe27，Gly31]-β-EP（II）。肽I和II显示出含有比β-内啡肽高2-2.5倍的阿片受体结合活性。我们还合成了两种具有还原烷基化半胱氨酸残基的类似物，这些肽，[Arg9,19,24,28,29 Cys(Cam)11,26,Phe27,Gly31]和[Arg9,19,24,28,29,Cys-(Cam)12,26,Phe27,Gly31]，显示出与β-内啡肽大致相同的阿片受体活性。
Zotero 插件