Easy Strategy To Protect Antimicrobial Peptides from Fast Degradation in Serum
2010 ◽
Vol 54
(9)
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pp. 4003-4005
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Keyword(s):
ABSTRACT Antimicrobial peptides are promising novel peptide leads, but their low serum stability often limits their further consideration in drug development programs. Here, we describe a generally applicable strategy to stabilize peptides against serum proteases by replacing arginine residues with α-amino-3-guanidino-propionic acid (Agp). Peptide NH2-RRWRIVVIRVRR-CONH2 was nearby totally degraded after 8 h in mouse serum, whereas the variant with Agp substituted was degraded less than 20%. The antimicrobial activity was not affected.