Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
- Resource Type
- Authors
- Rene B Khan; Linda A. Bester; Beatriz G. de la Torre; Estelle J. Ramchuran; Miguel Viñas; Fernando Albericio; Isabel Pérez-Guillén
- Source
- Digital.CSIC: Repositorio Institucional del CSIC
Consejo Superior de Investigaciones Científicas (CSIC)
Antibiotics
Volume 10
Issue 6
Dipòsit Digital de la UB
Universidad de Barcelona
Digital.CSIC. Repositorio Institucional del CSIC
instname
Antibiotics, Vol 10, Iss 695, p 695 (2021)
- Subject
- Microbiology (medical)
Solid-phase synthesis
Antimicrobial peptides
Peptide
Antibiòtics
RM1-950
010402 general chemistry
01 natural sciences
Biochemistry
Microbiology
Article
antimicrobial peptides
Gram-positive
Solid-phase peptide synthesis
Antibiotics
Pharmacology (medical)
General Pharmacology, Toxicology and Pharmaceutics
Cytotoxicity
Antibacterial agent
Antimicrobial synthesis
Therapeutic index
chemistry.chemical_classification
biology
010405 organic chemistry
Bacteris gramnegatius
biology.organism_classification
Antimicrobial
Síntesi en fase sólida
Gram-negative
0104 chemical sciences
Multiple drug resistance
Infectious Diseases
chemistry
therapeutic index
Gram-negative bacteria
solid-phase peptide synthesis
Therapeutics. Pharmacology
Pèptids
Antibacterial activity
Peptides
Bacteria
- Language
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.
The work was funded in part by the Marató TV3 Foundation 2018 (#20183530) and the National Research Foundation (NRF) (Blue Sky’s Research Programme # 120386).