Structure-activity relationship of mastoparan analogs: Effects of the number and positioning of Lys residues on secondary structure, interaction with membrane-mimetic systems and biological activity
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- 作者：Bibiana Monson de Souzaa ; f ; Marcia Perez dos Santos Cabrerab ; Paulo Cesar Gomesc ; f ; Nathalia Baptista Diasa ; f ; Rodrigo Guerino Stabelid ; Natalia Bueno Leitee ; Joã ; o Ruggiero Netoe ; Mario Sergio Palmaa ; f ; mspalma@rc.unesp.br" class="auth_mail" title="E-mail the corresponding author
- 关键词：Mastoparan ; Wasp venom ; Structure&ndash ; activity relationship ; Antimicrobial activity ; Peptide synthesis
- 刊名：Peptides
- 出版年：2015
- 出版时间：October 2015
- 年：2015
- 卷：72
- 期：Complete
- 页码：164-174
- 全文大小：2184 K
文摘
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Mastoparans are used as models for development of novel antimicrobial drugs.
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Mastoparan analogs were engineered based using strategies of Ala and Lys scanning.
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Ten synthetic mastoparans presenting from zero to six Lys residues were synthesized.
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Antibiotic activity of analogs was dependent on the extension of hydrophilic surface.
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Mast cell degranulation was dependent of Lys residues at positions 8 and/or 9.