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Issue 26, 2013
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AApeptides as a new class of antimicrobial agents

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Antibiotic resistance is an increasing public health concern around the world, and is recognized as one of the greatest threats facing humankind in the 21st century. Natural antimicrobial peptides (AMPs) are small cationic amphiphilic peptides found in virtually all living organisms, and play a key role in the defense against bacterial infections. Compared with conventional antibiotics, which target specific metabolic processes, AMPs are able to adopt globally amphipathic conformations, and kill bacteria through disruption of their membranes. As such, AMPs do not readily induce drug-resistance. However, AMPs are associated with intrinsic drawbacks such as low-to-moderate activity, susceptibility to enzymatic degradation, and inconvenience for optimization. Recently, we have developed a new class of peptidomimetics termed “AApeptides”. Such peptide mimics are highly resistant to protease degradation and are straightforward for chemical diversification and development. Our current studies show that AApeptides with globally amphipathic structures can mimic the bactericidal mechanism of AMPs, and display potent and broad-spectrum activity against both Gram-positive and -negative multi-drug-resistant bacteria. In this review, we summarize our current findings of antimicrobial AApeptides, and discuss potential future directions on the development of more potent and specific analogues.

Graphical abstract: AApeptides as a new class of antimicrobial agents

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Publication details

The article was received on 05 Mar 2013, accepted on 02 May 2013 and first published on 02 May 2013

Article type: Perspective
DOI: 10.1039/C3OB40444G
Org. Biomol. Chem., 2013,11, 4283-4290

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    AApeptides as a new class of antimicrobial agents

    Y. Niu, H. Wu, Y. Li, Y. Hu, S. Padhee, Q. Li, C. Cao and J. Cai, Org. Biomol. Chem., 2013, 11, 4283
    DOI: 10.1039/C3OB40444G

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