SYNTHESIS AND CHARACTERIZATION OF A DISULFIDE BOND ISOMER OF OMEGA-CONOTOXIN GVIA

被引：13

作者：

PENNINGTON, MW ^{[1
]}

FESTIN, SM ^{[1
]}

MACCECCHINI, ML ^{[1
]}

KEM, WR ^{[1
]}

机构：

[1] UNIV FLORIDA,COLL MED,DEPT PHARMACOL & THERAPEUT,GAINESVILLE,FL 32610

来源：

TOXICON | 1992年 / 30卷 / 07期

关键词：

D O I：

10.1016/0041-0101(92)90009-T

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Solid phase peptide synthesis and air oxidation of omega-conotoxin GVIA yielded, in addition to the desired product, an isomeric peptide which could be completely separated from the native toxin by repeated HPLC. A chymotrypsin-trypsin digest of this peptide, when subjected to HPLC peptide mapping, provided peptides identical with synthetic disulfide containing peptides predicted for the omega-conotoxin isomer containing C1-C2, C3-C5, C4-C6 cystinyl pairings. The 'shaking' potency (ED50 = 1500 pmoles/kg, i.c.v.) of the isomeric peptide upon cannulated rats was 1.3% of the potency of native conotoxin (ED50 = 20 pmoles/kg). Considering that all three disulfide pairings in the isomer are different from the native toxin, its retention of biological activity is of interest.

引用

页码：755 / 764

页数：10

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