Easy Strategy To Protect Antimicrobial Peptides from Fast Degradation in Serum-Reference-Cited by-同舟云学术

Easy Strategy To Protect Antimicrobial Peptides from Fast Degradation in Serum

Published:2010-09 Issue:9 Volume:54 Page:4003-4005
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Knappe Daniel¹,Henklein Petra²,Hoffmann Ralf¹,Hilpert Kai³

Affiliation:

1. Institute for Bioanalytical Chemistry, Center for Biotechnology and Biomedicine (BBZ), Faculty of Chemistry and Mineralogy, Universität Leipzig, Deutscher Platz 5, D-04103 Leipzig, Germany

2. Humboldt University of Berlin, Charité Berlin, Monbijoustrasse 2, D-10117 Berlin, Germany

3. Karlsruhe Institute of Technology (KIT), Institute of Functional Interfaces, P.O.B. 3640, D-76021 Karlsruhe, Germany

Abstract

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 NH 2 -RRWRIVVIRVRR-CONH 2 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.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.00300-10

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