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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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Detalles Bibliográficos
Autores principales: Ramchuran, Estelle J., Pérez-Guillén, Isabel, Bester, Linda A., Khan, René, Albericio, Fernando, Viñas, Miguel, de la Torre, Beatriz G.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8228121/
https://www.ncbi.nlm.nih.gov/pubmed/34200662
http://dx.doi.org/10.3390/antibiotics10060695
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author Ramchuran, Estelle J.
Pérez-Guillén, Isabel
Bester, Linda A.
Khan, René
Albericio, Fernando
Viñas, Miguel
de la Torre, Beatriz G.
author_facet Ramchuran, Estelle J.
Pérez-Guillén, Isabel
Bester, Linda A.
Khan, René
Albericio, Fernando
Viñas, Miguel
de la Torre, Beatriz G.
author_sort Ramchuran, Estelle J.
collection PubMed
description 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)(2)KLLKLL-NH(2) (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.
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spelling pubmed-82281212021-06-26 Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents Ramchuran, Estelle J. Pérez-Guillén, Isabel Bester, Linda A. Khan, René Albericio, Fernando Viñas, Miguel de la Torre, Beatriz G. Antibiotics (Basel) Article 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)(2)KLLKLL-NH(2) (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. MDPI 2021-06-10 /pmc/articles/PMC8228121/ /pubmed/34200662 http://dx.doi.org/10.3390/antibiotics10060695 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Ramchuran, Estelle J.
Pérez-Guillén, Isabel
Bester, Linda A.
Khan, René
Albericio, Fernando
Viñas, Miguel
de la Torre, Beatriz G.
Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
title Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
title_full Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
title_fullStr Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
title_full_unstemmed Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
title_short Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
title_sort super-cationic peptide dendrimers—synthesis and evaluation as antimicrobial agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8228121/
https://www.ncbi.nlm.nih.gov/pubmed/34200662
http://dx.doi.org/10.3390/antibiotics10060695
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