A human .alpha.-defensin 5 variant is obtained by adding amino acid residues at C-terminal of .alpha.-defensin 5 and then being modified to link an aliphatic acid. At least one of the added amino acid residues has a free amino group, and the free amino group is modified to link an aliphatic acid with 8-24 carbon atoms. The variant is used in manufacture of an antibacterial agent and an immunomodulatory agent. Antibacterial activity is significantly enhanced by extending and modifying the C-terminal of HD-5; in particular, salt tolerance is significantly improved by extending the C-terminal of HD-5 with Lys and then being modified with myristic acid, thereby breaking the restriction of salt-sensibility of conventional antimicrobial peptides. The variant can significantly promote release of inflammatory factors from macrophages and thus can be applied in manufacture of immunomodulatory agent.

Zhejiang University

Human alpha-defensin 5 variant and uses thereof

Disclosed are peptides having biological and therapeutic activity. Particularly disclosed are lipidated di- or tri-peptides analogs of KPV or KdPT that exhibit antimicrobial activity. In particular, the peptides of this invention provide enhanced anti-microbial activity over the base tri-peptides, lysine-proline-valine and lysine-d-proline-tyrosine. The disclosed peptides have the general formula of C12-18 lipid-KXZ-NH.sub.2i wherein K is lysine; X is proline, d-proline, histidine or arginine; Z is optional and if present Z is valine, threonine, alanine or leucine; and the terminal COOH is NH.sub.2 amidated. The C12-18 lipid is preferably the lipid moiety of lauric acid (C12), myristic acid (C14), pentadecanoic acid (C15), palmitic acid (C16), or stearic acid (C18). The invention is further related to methods of using of these peptides to treat various insults, inflammations or bacterial infections affecting the skin and other related mucosal body surfaces such as the oral cavity.

myristic acid/radang

Human alpha-defensin 5 variant and uses thereof

Short antimicrobial lipopeptides

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