期刊
AMINO ACIDS
卷 37, 期 2, 页码 285-295出版社
SPRINGER
DOI: 10.1007/s00726-008-0145-3
关键词
Chemotaxis; fMLF analogues; Formylpeptides; Human neutrophils; Tetrapeptides
资金
- Banca del Sangue di Ferrara for providing fresh blood and Fondazione Cassa di Risparmio di Ferrara
A small library of N-For and N-Boc tetrapeptidic analogues of the chemotactic tripeptide For-Met-Leu-Phe-OMe (fMLF-OMe), obtained by incorporating three different spacer aminoacids (Gly, beta Ala and Pro) between the native residues of Met and Leu (N-For- and N-Boc-Met-Xaa-Leu-Phe-OMe; Xaa(2) series) and Leu and Phe (N-For- and N-Boc-Met-Leu-Xaa-Phe-OMe; Xaa(3) series), have been synthesized and examined for their biological activity as agonists and antagonists. Chemotaxis, lysozyme release and superoxide anion production have been measured. All the N-For analogues maintain good to moderate chemotactic activity with the beta Ala(3) 15 model reaching the maximum value. All the N-Boc tetrapeptides are efficient chemotactic antagonists. Conversely, with the exception of the moderate antagonistic activity exhibited by the N-Boc Xaa(2) models against lysozyme release, all the other N-Boc analogues do not show significant activity against both superoxide anion and lysozyme release.
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