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Synthesis and biological properties of the seven alanine‐modified analogues of the marine cyclopeptide hymenamide C
Author(s) -
Napolitano Assunta,
Bruno Ines,
Rovero Paolo,
Lucas Rut,
Payà Peris Miguel,
GomezPaloma Luigi,
Riccio Raffaele
Publication year - 2002
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.396
Subject(s) - biological activity , elastase , peptide , degranulation , chemistry , alanine , stereochemistry , amino acid , combinatorial chemistry , biochemistry , computational biology , biology , in vitro , enzyme , receptor
The synthesis and biological activity of the marine cyclopeptide hymenamide C(1), showing an inhibitory effect on human neutrophil elastase degranulation release, were recently described. Based on this result, it was decided to undertake a systematic structure–activity relationship study of this cyclopeptide, based on the Ala‐scan technique, in order to obtain useful information for the rational design of additional analogues. The synthesis and characterization of the seven Ala modified analogues are reported and their biological and pharmacological properties are described. Copyright © 2002 European Peptide Society and John Wiley & Sons, Ltd.