Substrate based peptide aldehyde inhibits bacterial type I signal peptidase

作者：Buzder Lantos Peter; Bockstael Katrijn; Anne Jozef; Herdewijn Piet^*

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(10): 2880-2883.

DOI：10.1016/j.bmcl.2009.03.064

• Signal peptidase
• Antibiotics
• Peptides
• Structure-activity relationship

Bacterial type I signal peptidase is a potential target for the development of novel antibacterial agents. In this study we demonstrate that a substrate based peptide aldehyde inhibits signal peptidases with a lower IC(50) value than the lipopeptides described to date. The length of the core lipopeptide could be reduced by removing several amino acids from both termini. Conversion of this peptide to an aldehyde resulted in a molecule with an IC(50) value of 0.09 mu M when tested against Saccharomyces aureus SPase I, SpsB.

• 出版日期2009-5-15
• 单位河北医科大学