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Curr Med Chem. 2017 Nov 6. doi: 10.2174/0929867324666171107095913. [Epub ahead of print]

γ-AApeptides as a new strategy for therapeutic development.

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University of South Florida, - Department of Chemistry Tampa. United States.


A new class of peptidomimetics termed "γ-AApeptides" was recently developed by our group. Similar to other peptidomimetics, γ-AApeptides are resistant to proteolytic degradation, and possess limitless potential to introduce chemically diverse functional groups. γ-AApeptides have shown great promise in biomedical applications. In this article, we will review a few examples of γ-AApeptides with biological potential. Certain γ-AApeptides can permeate cell membranes and therefore they can be used as potential drug carrier. γ-AApeptides can also bind to HIV RNA with high specificity and affinity, suggesting their potential application as anti-HIV agents. Moreover, they can mimic host-defense peptides and display potent and broad-spectrum activity towards a range of drug-resistant bacterial pathogens. They are also potential anti-cancer agents. For instance, they have shown great promise in targeted imaging of tumor in mouse model, and they are also capable of disrupting p53/DNA interactions, and thus antagonize STAT3 signaling pathway. Recently, from combinatorial screening, γ-AApeptides are identified to inhibit A peptide aggregation, and thus they can be developed into potential anti-Alzheimer's Disease agent.


-AApeptides; Anti-Aaggregation.; Anti-HIV activity; Anticancer activity; Antimicrobial activity; Peptidomimetics; Structures

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