期刊
AMINO ACIDS
卷 43, 期 6, 页码 2279-2283出版社
SPRINGER WIEN
DOI: 10.1007/s00726-012-1305-z
关键词
Antimicrobial peptide; Difficult sequence; Haemolytic activity; Gonococcal growth inhibitor 1; Solid phase peptide synthesis
资金
- Victorian Government's Operational Infrastructure Support Program
Gonococcal growth inhibitor 1 (GGI-1) is a 44-residue peptide with potent anti-Legionella activity. It has been isolated from Staphylococcus haemolyticus but, to date, its chemical synthesis has not been reported. Acquisition of this peptide via this means would enable a more detailed examination of its antimicrobial properties. However, its synthesis represents a significant challenge because of two predicted difficult sequences within the peptide. Its successful solid-phase assembly is reported in this paper, and was accomplished by use of simple palliative measures including the introduction of a single pseudo-proline isostere in order to counteract on-resin aggregation. The peptide had moderate antimicrobial activity against Escherichia coli but was inactive against another Gram-negative bacterium and two Gram-positive bacteria (Bacillus species). It had significant haemolytic activity, with a H-50 (concentration of peptide that causes 50 % haemolysis) of 20 and 125 mu M for two blood samples from different donors. An alternative therapeutic index to that proposed for GGI-1 in a recent publication is proposed.
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