Rationally Modified Antimicrobial Peptides from the N-Terminal Domain of Human RNase 3 Show Exceptional Serum Stability

Multidrug resistance against conventional antibiotics poses an important threat to human health. In this context, antimicrobial peptides (AMPs) have been extensively studied for their antibacterial activity and promising results have been shown so far. However, AMPs tend to be rather vulnerable to p...

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Detalles Bibliográficos
Autores: Sandín, Daniel|||0000-0002-2805-0208, Valle García, Javier|||0000-0002-6787-8286, Chaves-Arquero, Belén, Prats-Ejarque, Guillem|||0000-0002-8213-4947, Larrosa, María Nieves|||0000-0001-8808-0233, González-López, Juanjo|||0000-0003-2419-5909, Jiménez, María Ángeles|||0000-0001-6835-5850, Boix, Ester|||0000-0003-1790-2142, Andreu Martínez, David|||0000-0002-6317-6666, Torrent, Marc|||0000-0001-6567-3474
Tipo de recurso: artículo
Fecha de publicación:2021
País:España
Institución:Universitat Autònoma de Barcelona
Repositorio:Dipòsit Digital de Documents de la UAB
Idioma:inglés
OAI Identifier:oai:ddd.uab.cat:250444
Acceso en línea:https://ddd.uab.cat/record/250444
https://dx.doi.org/urn:doi:10.1021/acs.jmedchem.1c00795
Access Level:acceso abierto
Palabra clave:Serum
Peptides and proteins
Antimicrobial activity
Bacteria
Toxicity
Descripción
Sumario:Multidrug resistance against conventional antibiotics poses an important threat to human health. In this context, antimicrobial peptides (AMPs) have been extensively studied for their antibacterial activity and promising results have been shown so far. However, AMPs tend to be rather vulnerable to protease degradation, which offsets their therapeutic appeal. Here, we demonstrate how replacing functional residues in the antimicrobial region of human RNase 3-also named eosinophil cationic protein-by non-natural amino acids increases stability in human serum. These changes were also shown to reduce the hemolytic effect of the peptides in general terms, whereas the antimicrobial activity was reasonably preserved. Digestion profiles enabled us to design new peptides with superior stability and lower toxicity that could become relevant candidates to reach clinical stages.