Improvement of Bacterial Cell Selectivity of Melittin by a Single Trp Mutation with a Peptoid Residue

Title: Improvement of Bacterial Cell Selectivity of Melittin by a Single Trp Mutation with a Peptoid Residue

Volume: 13 Issue: 7

Author(s): Wan Long Zhu, Yoonkyung Park, Il-Seon Park, Yong Sun Park, Yangmee Kim, Kyung-Soo Hahm and Song Yub Shin

Affiliation:

Keywords: Melittin, Trp-peptoid residue (Nhtrp), cell selectivity, helical assembly, structural flexibility

Abstract: To design melittin (ME) analogues that are not cytotoxic against mammalian cells but which possessing potent antimicrobial activity, we synthesized a ME analogue (ME-w) in which the Trp-19 residue of ME was replaced by a Trppeptoid residue (Nhtrp). ME-w exhibited similar antimicrobial activity compared to ME against the tested six bacteria and C. albicans. However, it was much less cytotoxic against the hRBCs and HeLa and NIH-3T3 cells than ME. Tryptophan fluorescence and CD spectra revealed that the Trp-19 ® Nhtrp substitution in ME contributed to a much lower helical assembly in an aqueous environment and structural flexibility and exterior localization to zwitterionic membrane which modulates its selectivity toward bacterial cells.

Cite this article as:

Long Zhu Wan, Park Yoonkyung, Park Il-Seon, Sun Park Yong, Kim Yangmee, Hahm Kyung-Soo and Yub Shin Song, Improvement of Bacterial Cell Selectivity of Melittin by a Single Trp Mutation with a Peptoid Residue, Protein & Peptide Letters 2006; 13 (7) . https://dx.doi.org/10.2174/092986606777790575

DOI https://dx.doi.org/10.2174/092986606777790575	Print ISSN 0929-8665
Publisher Name Bentham Science Publisher	Online ISSN 1875-5305