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人生长激素(6 - 13)降血糖类似物的结构与体内活性

Structure and in vivo activity of hypoglycaemic analogues of human growth hormone (6-13).

作者信息

Thompson P, Lim N, Ede N J, Ng F M, Rae I D, Hearn M T

机构信息

Department of Biochemistry and Molecular Biology, Monash University, Clayton, Australia.

出版信息

Drug Des Discov. 1995 Aug;13(1):55-72.

PMID:8882901
Abstract

A range of peptide analogues related to Asu11-human growth hormone (6-13) have been synthesized and tested for hypoglycaemic activity using in vivo insulin tolerance tests. Utilising an alanine scan procedure and a selective amino acid residue approach these structure-activity studies suggest that residues Phe10, Arg8 and the C-terminal beta-turn structure are important for the expression of biological activity.

摘要

已经合成了一系列与天冬酰胺-11-人生长激素(6-13)相关的肽类似物,并使用体内胰岛素耐量试验测试了它们的降血糖活性。利用丙氨酸扫描程序和选择性氨基酸残基方法,这些构效关系研究表明,苯丙氨酸10、精氨酸8残基和C末端β-转角结构对于生物活性的表达很重要。

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