Antimicrobial activities and action mechanism studies of transportan 10 and its analogues against XXXX .

@entity1 @entity6371 @entity137 @entity281 @entity580
UNASSIGNED: The increased emergence of @entity6371 is perceived as a critical public health threat, creating an urgent need for the development of novel classes of antimicrobials. Cell-penetrating peptides that share common features with antimicrobial peptides have been found to have antimicrobial activity and are currently being considered as potential alternatives to antibiotics. Transportan 10 is a chimeric cell-penetrating peptide that has been reported to transport biologically relevant cargoes into @entity1 cells and cause damage to microbial membranes. In this study, we designed a series of TP10 analogues and studied their structure-activity relationships. We first evaluated the antimicrobial activities of these compounds against @entity6371 , which are responsible for most @entity580 . Our results showed that several of these compounds had potent antimicrobial and biofilm-inhibiting activities. We also measured the @entity137 of these compounds, finding that Lys substitution could increase the antimicrobial activity but significantly enhanced the @entity137 . Pro introduction could reduce the @entity137 but disrupted the helical structure, resulting in a loss of activity. In the mechanistic studies, TP10 killed bacteria by membrane-active and DNA-binding activities. In conclusion, TP10 and its analogues could be developed into promising antibiotic candidates for the treatment of @entity281 caused by @entity6371 . Copyright    2015 European Peptide Society and John Wiley _ Sons, Ltd.
