PMID: 11445228Jul 11, 2001Paper

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

Peptides
Rajiv Grover, Stefan 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)

References

May 26, 1997·European Journal of Pharmacology·A MüllerS Dhein
Jul 1, 1997·Naunyn-Schmiedeberg's Archives of Pharmacology·A MüllerS Dhein
Jan 1, 1964·Circulation Research·J HAN, G K MOE

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Citations

Nov 28, 2009·Naunyn-Schmiedeberg's Archives of Pharmacology·Stefan DheinFriedrich-Wilhelm Mohr
Sep 12, 2012·Naunyn-Schmiedeberg's Archives of Pharmacology·Joanna JozwiakStefan Dhein
Jul 21, 2007·Journal of Huazhong University of Science and Technology. Medical Sciences = Hua Zhong Ke Ji Da Xue Xue Bao. Yi Xue Ying De Wen Ban = Huazhong Keji Daxue Xuebao. Yixue Yingdewen Ban·Rong WangLin Wang
Sep 10, 2002·Peptides·Stefan Dhein
Dec 2, 2006·Nature Reviews. Drug Discovery·Stanley Nattel, Leif Carlsson
Jan 30, 2009·Cardiovascular Research·Anja HagenStefan Dhein
Jun 4, 2004·Journal of Cardiovascular Pharmacology·Ketil HauganJørgen Søberg Petersen
Dec 19, 2003·Cell Communication & Adhesion·Stefan DheinFriedrich-Wilhelm Mohr
Jul 25, 2009·Cell Communication & Adhesion·Xiao-Qing QuanCun-Tai Zhang
Jan 27, 2011·British Journal of Pharmacology·Elke De VuystLuc Leybaert
Jun 18, 2002·Cell Communication & Adhesion·S DheinL Polontchouk
Sep 22, 2017·Pharmacological Reviews·Luc LeybaertRainer Schulz

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