論文 - 詳細
| RRC ID | 84798 |
|---|---|
| 著者 | Hashizume H, Sawa R, Kubota Y, Adachi S, Harada S, Igarashi M. |
| タイトル | Precursor-directed biosynthesis and biological activity of tripropeptin Cpip, a new tripropeptin C analog containing pipecolic acid. |
| ジャーナル | J Antibiot (Tokyo) |
| Abstract |
Tripropeptin C, a non-ribosomal cyclic lipopeptide containing three proline residues, exhibits excellent efficacy in the mouse-methicillin-resistant Staphylococcus aureus septicemia model. Since tripropeptins contain L-prolyl-D-proline and, as a result, are known to form a hairpin structure in proteins, it was of interest to determine whether this substructure contributes to their antibacterial activity. In this study, prolines in tripropeptin C were replaced with pipecolic acid(s) using precursor-directed biosynthesis. Only a new tripropeptin analog, tripropeptin Cpip, which has one L-pipecolic acid in place of L-proline, was isolated. The in vitro antimicrobial activity of the new analog was approximately two to four times weaker activity against Gram-positive bacteria, including drug-resistant species, compared with that of tripropeptin C. These results suggest that the L-prolyl-D-proline substructure plays an important role in the observed potency of tripropeptins. |
| 巻・号 | 77(4) |
| ページ | 238-244 |
| 公開日 | 2024-4-1 |
| DOI | 10.1038/s41429-024-00703-9 |
| PII | 10.1038/s41429-024-00703-9 |
| PMID | 38267574 |
| MeSH | Animals Anti-Bacterial Agents / chemistry Inositol Phosphates* Lipopeptides Methicillin-Resistant Staphylococcus aureus* / metabolism Mice Microbial Sensitivity Tests Pipecolic Acids* Proline Prostaglandins E* |
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| 最多言及媒体 | X(Twitter) |
| 各媒体での言及数の合計 | 1 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| 一般微生物 | JCM5803 JCM5804 |