ArticleACS medicinal chemistry letters2015
Structure-Activity Relationship Studies of 3-epi-Deoxynegamycin Derivatives as Potent Readthrough Drug Candidates.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Negamycin: Nature's Forgotten Antibiotic.ACS infectious diseases · 2026Review
- A heme-dependent enzyme forms the hydrazine in the antibiotic negamycin.Nature chemical biology · 2025Article
- Development of Conformationally Restricted Negamycin Derivatives for Potent Readthrough Activity.ACS medicinal chemistry letters · 2023Article
- New Negamycin-Based Potent Readthrough Derivative Effective against TGA-Type Nonsense Mutations.ACS medicinal chemistry letters · 2019Article
- Chemotherapeutics overcoming nonsense mutation-associated genetic diseases: medicinal chemistry of negamycin.The Journal of antibiotics · 2018Review
- Structure-Activity Relationship Study of Leucyl-3-ACS medicinal chemistry letters · 2017Article
- Clinical potential of ataluren in the treatment of Duchenne muscular dystrophy.Degenerative neurological and neuromuscular disease · 2016Review
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
(+)-Negamycin (1), a natural dipeptidic antibiotic bearing a hydrazide structure, exhibits a readthrough activity toward the nonsense mutation of the dystrophin gene and restores dystrophin expression in muscles of Duchenne muscular dystrophy model mdx mice. Herein to develop more potent readthrough compounds, we performed a structure-activity relationship (SAR) study of 3-epi-deoxynegamycin (2), which is also another natural readthrough compound with little antimicrobial activity, focusing on the main carbon chain length. We found that one carbon atom shorter derivative 9b shows a higher readthrough activity than 1 and 2. Further derivatization at the carboxylic acid part of 9b demonstrates that its meta-chlorobenzyl ester derivative 17e, which has a higher ClogP value, exhibits a more potent readthrough activity than 9b. Interestingly, in the cell-free protein expression system, the readthrough activity of 17e drastically decreases compared to that in the cell-based assay. These results suggest that benzyl ester-type derivatives enhance the hydrophobicity and function as prodrugs to produce active compound 9b in living cell systems.
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