AI Article Synopsis
- * The study focused on creating Fmoc-triazine amino acids with different chemical properties for better AMP formulations, leading to the synthesis of new amphipathic peptidomimetics.
- * The most effective compound identified was a trimer that not only exhibited strong antimicrobial activity without harming red blood cells but also showed improved stability against proteolytic degradation and targeted bacteria internally.*
Article Abstract
To combat the escalating rise of antibacterial resistance, the development of antimicrobial peptides (AMPs) with a unique mode of action is considered an attractive strategy. However, proteolytic degradation of AMPs remains the greatest challenge in their transformation into therapeutics. Herein, we synthesized Fmoc-triazine amino acids that differ from each other by anchoring either cationic or hydrophobic residues. These unnatural amino acids were adopted for solid-phase peptide synthesis (SPPS) to synthesize a series of amphipathic antimicrobial peptidomimetics. From the antimicrobial screening, we found that the trimer, is the most potent short antimicrobial peptidomimetic without showing hemolytic activity and it displayed enhanced proteolytic stability. Moreover, the mechanism of action to kill bacteria was found to be an intracellular targeting.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7279249 | PMC |
| http://dx.doi.org/10.3390/ijms21103602 | DOI Listing |
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