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Synthesis of Fmoc-Triazine Amino Acids and Its Application in the Synthesis of Short Antibacterial Peptidomimetics.

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, BJK-4 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.

journal_name

Int J Mol Sci

journal_title

International journal of molecular sciences

authors

Gunasekaran P,Kim EY,Lee J,Ryu EK,Shin SY,Bang JK

doi

10.3390/ijms21103602

subject

Has Abstract

pub_date

2020-05-20 00:00:00

issue

10

issn

1422-0067

pii

ijms21103602

journal_volume

21

pub_type

杂志文章

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