9J1M9J1M の概要
| エントリーDOI | 10.2210/pdb9j1m/pdb |
| EMDBエントリー | 61076 |
| 分子名称 | Large ribosomal subunit protein bL32, Large ribosomal subunit protein uL3, Large ribosomal subunit protein uL4, ... (55 entities in total) |
| 機能のキーワード | ribosome, macrolide, antibiotic, ribosome-antibiotic complex, ribosome/antibiotic |
| 由来する生物種 | Mycobacterium tuberculosis variant bovis BCG str. Pasteur 1173P2 詳細 |
| タンパク質・核酸の鎖数 | 52 |
| 化学式量合計 | 2247404.10 |
| 構造登録者 | |
| 主引用文献 | Isozaki, Y.,Makikawa, T.,Kimura, K.,Nishihara, D.,Fujino, M.,Tanaka, Y.,Hayashi, C.,Ishizaki, Y.,Igarashi, M.,Yokoyama, T.,Toshima, K.,Takahashi, D. Creation of a macrolide antibiotic against non-tuberculous Mycobacterium using late-stage boron-mediated aglycon delivery. Sci Adv, 11:eadt2352-eadt2352, 2025 Cited by PubMed Abstract: Non-tuberculous mycobacteria (NTM) is gaining clinical recognition as a recently emerging pulmonary pathogen. complex (MAC), the most common NTM, is the cause of pulmonary MAC disease. Currently, the macrolide azithromycin (AZM) is the standard first-line antibiotic for treatment of the disease. However, the rise of drug-resistant MAC necessitates the development of alternative therapeutics. Here, we present a late-stage boron-mediated aglycon delivery strategy for selective modification of AZM, generating a library of potential anti-MAC drugs designated to . Screening of to revealed that exhibited enhanced antimicrobial activity against wild-type and macrolide-resistant MAC compared to AZM. Cryo-electron microscopy analysis indicated that the inserted tercyclic moiety of formed a robust anchor on the bacterial ribosome, creating a binding pocket with base flipping of U2847, potentially bypassing the standard mechanism of macrolide resistance. These results position as a promising lead for therapeutics against macrolide-resistant MAC. PubMed: 40043128DOI: 10.1126/sciadv.adt2352 主引用文献が同じPDBエントリー |
| 実験手法 | ELECTRON MICROSCOPY (2.33 Å) |
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