Examining topoisomers of a snake-venom-derived peptide for improved antimicrobial and antitumoral properties

Ctn[15-34], the C-terminal section of crotalicidin (Ctn), a cathelicidin from a South American pit viper, is an antimicrobial and antitumoral peptide with remarkably longer stability in human serum than the parent Ctn. In this work, a set of topoisomers of both Ctn and Ctn[15-34], including the retr...

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Detalles Bibliográficos
Autores: Carrera-Aubesart, Adam, Defaus, Sira, Pérez-Peinado, Clara, 1991-, Sandín, Daniel, Torrent Burgas, Marc, Jiménez, M. Ángeles, Andreu Martínez, David
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:España
Institución:Universitat Pompeu Fabra
Repositorio:Repositorio Digital de la UPF
OAI Identifier:oai:repositori.upf.edu:10230/54847
Acceso en línea:http://hdl.handle.net/10230/54847
http://dx.doi.org/10.3390/biomedicines10092110
Access Level:acceso abierto
Palabra clave:Ctn[15-34]
Antimicrobial peptides
Antitumoral peptides
Crotalicidin
Enantio-, retro-, and retroenantio peptides
Snake venom
Topoisomer peptides
Descripción
Sumario:Ctn[15-34], the C-terminal section of crotalicidin (Ctn), a cathelicidin from a South American pit viper, is an antimicrobial and antitumoral peptide with remarkably longer stability in human serum than the parent Ctn. In this work, a set of topoisomers of both Ctn and Ctn[15-34], including the retro, enantio, and retroenantio versions, were synthesized and tested to investigate the structural requirements for activity. All topoisomers were as active as the cognate sequences against Gram-negative bacteria and tumor cells while slightly more toxic towards normal cells. More importantly, the enhanced serum stability of the D-amino-acid-containing versions suggests that such topoisomers must be preferentially considered as future antimicrobial and anticancer peptide leads.