Design, synthesis, and antiproliferative activities of stapled melittin peptides

Wu, Ye; Han, Meng-fei; Liu, Chao; Liu, Tai-yu; Feng, Yu-fei; Zou, Yan; Li, Bai; Liao, Hong-li

Design, synthesis, and antiproliferative activities of stapled melittin peptides

2017

Melittin is a 26-residue, amphipathic, cell-penetrating, α-helical anti-hepatoma peptide isolated from bee venom. However, the application of melittin as a drug is limited owing to its original conformational flexibility and low stability. In this study, we designed, synthesized, and tested a series of hydrocarbon-stapled analogs of melittin, of which, some analogs showed remarkable enhancement not only in anti-hepatoma activity, but also in α-helicity and protease resistance when compared to the parent melittin. These results disclosed the important impact of all-hydrocarbon crosslinking on the biological activity, stability, and hemolytic activity of melittin.

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