[DES HIS(1), DES PHE(6), GLU(9)]GLUCAGON AMIDE - A NEWLY DESIGNED PURE GLUCAGON ANTAGONIST

被引：18

作者：

AZIZEH, BY ^{[1
]}

VANTINE, BA ^{[1
]}

STURM, NS ^{[1
]}

HUTZLER, AM ^{[1
]}

DAVID, C ^{[1
]}

TRIVEDI, D ^{[1
]}

HRUBY, VJ ^{[1
]}

机构：

[1] UNIV ARIZONA,DEPT CHEM,TUCSON,AZ 85721

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 16期

关键词：

D O I：

10.1016/0960-894X(95)00307-F

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the synthesis and biological activity of a new glucagon analog that was designed as a glucagon receptor antagonist by appropriate modifications in the N-terminal region of glucagon. The structure of the new analog is [des His(1), des Phe(6), Glu(9)]glucagon amide, and its binding potency IC50 value of 48 nM. The compound was found to be a pure antagonist in a new much more sensitive assay for glucagon stimulated cAMP accumulation activity and showed a pA(2) value of 8.20 in this assay.

引用

页码：1849 / 1852

页数：4

共 24 条

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