Literature DB >> 11445228

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

R Grover1, S Dhein.   

Abstract

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-NH(2)) 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[CF(3)C(OH)-Gly-Ala-Gly-Hyp-Pro-Tyr] showed promising activities. (supported by the DFG and Köln-Fortune)

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Year:  2001        PMID： 11445228     DOI： 10.1016/s0196-9781(01)00419-3

Source DB:  PubMed          Journal:  Peptides        ISSN： 0196-9781            Impact factor:   3.750


  8 in total

Review 1.  Improving cardiac gap junction communication as a new antiarrhythmic mechanism: the action of antiarrhythmic peptides.

Authors:  Stefan Dhein; Anja Hagen; Joanna Jozwiak; Anna Dietze; Jens Garbade; Markus Barten; Martin Kostelka; Friedrich-Wilhelm Mohr
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2009-11-27       Impact factor: 3.000

Review 2.  Pharmacological modulation of connexin-formed channels in cardiac pathophysiology.

Authors:  Elke De Vuyst; Kerstin Boengler; Gudrun Antoons; Karin R Sipido; Rainer Schulz; Luc Leybaert
Journal:  Br J Pharmacol       Date:  2011-06       Impact factor: 8.739

Review 3.  Connexins in Cardiovascular and Neurovascular Health and Disease: Pharmacological Implications.

Authors:  Luc Leybaert; Paul D Lampe; Stefan Dhein; Brenda R Kwak; Peter Ferdinandy; Eric C Beyer; Dale W Laird; Christian C Naus; Colin R Green; Rainer Schulz
Journal:  Pharmacol Rev       Date:  2017-10       Impact factor: 25.468

4.  Desipramine prevents cardiac gap junction uncoupling.

Authors:  Joanna Jozwiak; Anna Dietze; Rajiv Grover; Alex Savtschenko; Christian Etz; Friedrich W Mohr; Stefan Dhein
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2012-09-11       Impact factor: 3.000

5.  Local effects and mechanisms of antiarrhythmic peptide AAP10 in acute regional myocardial ischemia: electrophysiological and molecular findings.

Authors:  Joanna Jozwiak; Stefan Dhein
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2008-06-24       Impact factor: 3.000

6.  Changes in phosphorylation of connexin43 in rats during acute myocardial hypoxia and effects of antiarrhythmic peptide on the phosphorylation.

Authors:  Rong Wang; Cuntai Zhang; Yanfei Ruan; Nian Liu; Lin Wang
Journal:  J Huazhong Univ Sci Technolog Med Sci       Date:  2007-06

Review 7.  Mechanisms of Connexin Regulating Peptides.

Authors:  D Ryan King; Meghan W Sedovy; Xinyan Leng; Jianxiang Xue; Samy Lamouille; Michael Koval; Brant E Isakson; Scott R Johnstone
Journal:  Int J Mol Sci       Date:  2021-09-22       Impact factor: 5.923

8.  Regulation of gap junctions by nitric oxide influences the generation of arrhythmias resulting from acute ischemia and reperfusion in vivo.

Authors:  Agnes Végh; Márton Gönczi; Gottfried Miskolczi; Mária Kovács
Journal:  Front Pharmacol       Date:  2013-06-14       Impact factor: 5.810
  8 in total

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