Converting Teixobactin into a Cationic Antimicrobial Peptide (AMP)
| Autor: | Fernando Albericio, Shimaa A. H. Abdel Monaim, Beatriz G. de la Torre, Estelle J. Ramchuran, Ayman El-Faham |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
chemistry.chemical_classification
Bacteria 010405 organic chemistry Chemistry Stereochemistry Teixobactin Cationic polymerization Biological activity Peptide Bacterial Infections Microbial Sensitivity Tests 010402 general chemistry Antimicrobial 01 natural sciences 0104 chemical sciences Amino acid Anti-Bacterial Agents Depsipeptides mental disorders Drug Discovery Side chain Molecular Medicine Humans Antimicrobial Cationic Peptides |
| Zdroj: | Journal of medicinal chemistry. 60(17) |
| ISSN: | 1520-4804 |
| Popis: | Teixobactin is a head to side chain cyclodepsipeptide that contains two positive charges. One is found in the cycle, as a result of the presence of the guanidino-unusual amino acid L-allo-End, while the other is at the N-terminal. Here we introduce 26 new Teixobactin analogues with an increasing number of positive charges. In an attempt to fine-tune the biological activity of Teixobactin, we examined the effect of cationicity on the SAR of these analogues. The maximum number of positive charges to maintain the activity are three to four. Analogues with five positive charges show the lowest activity. |
| Databáze: | OpenAIRE |
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