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Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors
The efficacy of carbapenem antibiotics can be compromised by metallo-β-lactamases, but a high-throughput screen followed by optimization has now enabled the discovery of indole-2-carboxylates (InCs) as potent broad-spectrum metallo-β-lactamase inhibitors. The results highlight the potential of InC–carbapenem combinations for clinical use as well as mechanism-guided approaches to combatting globally disseminated antibiotic resistant mechanisms.
- Jürgen Brem
- , Tharindi Panduwawala
- & Christopher J. Schofield
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News & Views |
Designing in vivo active DNAzymes
The therapeutic applications of DNAzymes are limited because of their low effectiveness in vivo. Now, a promising approach for constructing DNAzymes that show high gene-silencing efficiency in mammalian cells has been developed. This approach incorporates chemical modifications into an existing DNAzyme scaffold.
- Yifei Zhou
- & Chuanzheng Zhou
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News & Views |
Straining to react
A new click-style reaction based on a strain-release amination strategy has been developed. This approach can be used to append small, strained ring systems onto a core scaffold.
- John A. Milligan
- & Peter Wipf