Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents

Microbial infections are a major public health concern. Antimicrobial peptides (AMPs) have been demonstrated to be a plausible alternative to the current arsenal of drugs that has become inefficient due to multidrug resistance. Herein we describe a new AMP family, namely the super-cationic peptide d...

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Bibliographic Details
Authors: Ramchuran, Estelle J., Pérez-Guillén, Isabel, Bester, Linda A., Khan, René, Albericio, Fernando, Viñas, Miguel, de la Torre, Beatriz G.
Format: article
Status:Published version
Publication Date:2021
Country:España
Institution:Consejo Superior de Investigaciones Científicas (CSIC)
Repository:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/247299
Online Access:http://hdl.handle.net/10261/247299
Access Level:Open access
Keyword:Solid-phase peptide synthesis
Antimicrobial synthesis
Gram-positive
Gram-negative
Therapeutic index
Description
Summary:Microbial infections are a major public health concern. Antimicrobial peptides (AMPs) have been demonstrated to be a plausible alternative to the current arsenal of drugs that has become inefficient due to multidrug resistance. Herein we describe a new AMP family, namely the super-cationic peptide dendrimers (SCPDs). Although all members of the series exert some antibacterial activity, we propose that special attention should be given to (KLK)2KLLKLL-NH2 (G1KLK-L2KL2), which shows selectivity for Gram-negative bacteria and virtually no cytotoxicity in HepG2 and HEK293. These results reinforce the validity of the SCPD family as a valuable class of AMP and support G1KLK-L2KL2 as a strong lead candidate for the future development of an antibacterial agent against Gram-negative bacteria.