The pharmacophore of short cationic antibacterial peptides.
Cationic antibacterial peptides have been proclaimed as new drugs against multiresistant bacteria. Their limited success so far is partially due to the size of the peptides, which gives rise to unresolved issues regarding administration, bioavailability, metabolic stability, and immunogenicity. We have systematically investigated the minimum antibacterial motif of cationic antibacterial peptides regarding charge and lipophilicity/bulk and found that the pharmacophore was surprisingly small, opening the opportunity for development of short antibacterial peptides for systemic use.
Strøm
Morten B
MB
Department of Chemistry, University of Tromsø, N-9037 Tromsø, Norway.
Haug
Bengt Erik
BE
Skar
Merete L
ML
Stensen
Wenche
W
Stiberg
Trine
T
Svendsen
John S
JS
D023181:Antimicrobial Cationic Peptides / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D024901:Drug Resistance, Multiple, Bacterial; D004926:Escherichia coli / Q000187:drug effects; D006461:Hemolysis; D006801:Humans; D008826:Microbial Sensitivity Tests; D010446:Peptide Fragments / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D023181:Antimicrobial Cationic Peptides; D010446:Peptide Fragments