TYR(13) IS ESSENTIAL FOR THE ACTIVITY OF OMEGA-CONOTOXIN MVIIA AND GVIA, SPECIFIC N-TYPE CALCIUM-CHANNEL BLOCKERS

被引：64

作者：

KIM, JI ^{[1
]}

TAKAHASHI, M ^{[1
]}

OHTAKE, A ^{[1
]}

WAKAMIYA, A ^{[1
]}

SATO, K ^{[1
]}

机构：

[1] MITSUBISHI KASEI INST LIFE SCI,MACHIDA 194,TOKYO,JAPAN

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1995年 / 206卷 / 02期

关键词：

D O I：

10.1006/bbrc.1995.1063

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Two analogs of cu-conotoxin MVIIA, a 25mer peptide neurotoxin, were synthesized by replacing Lys(2) or Tyr(13) with Ala. The activities of synthetic analogs were estimated from the inhibitory action on I-125-omega-conotoxin GVIA binding to chick brain synaptic plasma membranes. As in the case of omega-conotoxin GVIA, replacement of Tyr(13) resulted in an enormous reduction in activity. In contrast, substitution of Ala for Lys(2) gave only a small effect. These results indicate that Tyr(13) is a critical amino acid of omega-conotoxin MVIIA and GVIA for blocking N-type calcium channel function. (C) 1995 Academic Press, Inc.

引用

页码：449 / 454

页数：6

共 14 条

[1] STRUCTURE AND FUNCTION OF VOLTAGE-SENSITIVE ION CHANNELS [J].