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具有二硫键的人β-内啡肽类似物生物活性的合成

Synthesis of biological activity of human beta-endorphin analogs with disulfide bridges.

作者信息

Blake J, Chang W C, Li C H

出版信息

Int J Pept Protein Res. 1979;14(3):275-80. doi: 10.1111/j.1399-3011.1979.tb01933.x.

Abstract

Three analogs of human beta-endorphin containing internal cystine bridges have been synthesized and their biological activities have been determined. It was found that the analogs with disulfide bridges between positions 17 and 26 or 11 and 26 retained full opiate activity as estimated by guinea ileum assay, whereas the analog with a cystine bridge between positions 7 and 26 showed reduced opiate activity. None of the analogs retained significant immunoactivity as revealed by radioimmunoassay.

摘要

已合成了三种含内部胱氨酸桥的人β-内啡肽类似物,并测定了它们的生物活性。通过豚鼠回肠试验估计发现,在17位和26位或11位和26位之间具有二硫键桥的类似物保留了全部阿片活性,而在7位和26位之间具有胱氨酸桥的类似物显示出降低的阿片活性。放射免疫测定显示,这些类似物均未保留显著的免疫活性。

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