Structure-activity relationships of novel peptides related to the antiarrhythmic peptide AAP10 which reduce the dispersion of epicardial action potential duration

被引：33
|
作者：
Grover, R
Dhein, S
机构：
[1] Univ Halle Wittenberg, Inst Pharmacol, D-06097 Halle, Germany
[2] Univ Cologne, Inst Pharmacol, D-50931 Cologne, Germany
来源：
PEPTIDES | 2001年 / 22卷 / 07期
关键词：
antiarrhythmic peptide; clap junction; cardiac ischemia; structure-activity relationships;
D O I：
10.1016/S0196-9781(01)00419-3
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：
We report the first study on short peptide structure-activity relationships (SAR) for the antiarrhythmic peptide AAP10 and its putative receptor. Synthetic improvements on the natural antiarrhythmic peptide AAPnat (H-Gly-Pro-Hyp-Gly-Ala-Gly) isolated from bovine atria led us to the synthesis of our lead molecule AAP10 (H-Gly-Ala-Gly-Hyp-Pro-Tyr-NH2) which reduces dispersion of epicardial potential duration and acts antiarrhythmically in isolated rabbit hearts. The aim of our study was to elucidate structure-activity relationships for AAP10 based on Langendorff experiments and molecular modeling. Mutation of the amino acid sequence led to 11 different peptides which were tested analogous to the lead molecule. Among these new synthetic peptides various including the cyclopeptide cAAP10RG, cyclo[CF3C(OH)-Gly-Ala-Gly-Hyp-Pro-Tyr] showed promising activities. (supported by the DFG and Koln-Fortune) (C) 2001 Elsevier Science Inc. All rights reserved.
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收藏
页码：1011 / 1021
页数：11
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