Examining Topoisomers of a Snake-Venom-Derived Peptide for Improved Antimicrobial and Antitumoral Properties
| Autor: | Adam Carrera-Aubesart, Sira Defaus, Clara Pérez-Peinado, Daniel Sandín, Marc Torrent, Maria Ángeles Jiménez, David Andreu |
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| Jazyk: | angličtina |
| Rok vydání: | 2022 |
| Předmět: | |
| Zdroj: | Biomedicines, Vol 10, Iss 9, p 2110 (2022) |
| Druh dokumentu: | article |
| ISSN: | 10092110 2227-9059 |
| DOI: | 10.3390/biomedicines10092110 |
| Popis: | Ctn[15-34], the C-terminal section of crotalicidin (Ctn), a cathelicidin from a South American pit viper, is an antimicrobial and antitumoral peptide with remarkably longer stability in human serum than the parent Ctn. In this work, a set of topoisomers of both Ctn and Ctn[15-34], including the retro, enantio, and retroenantio versions, were synthesized and tested to investigate the structural requirements for activity. All topoisomers were as active as the cognate sequences against Gram-negative bacteria and tumor cells while slightly more toxic towards normal cells. More importantly, the enhanced serum stability of the D-amino-acid-containing versions suggests that such topoisomers must be preferentially considered as future antimicrobial and anticancer peptide leads. |
| Databáze: | Directory of Open Access Journals |
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