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Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors

Abstract:

Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1 inhibitors identified indole-2-carboxylates (InCs) as potential β-lactamase stable β-lactam mimics. Subsequent structure–activity relationship studies revealed InCs as a new class of potent MBL inhibitor, active against all MBL classes of major clinical relevan...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1038/s41557-021-00831-x

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Role:
Author
ORCID:
0000-0002-0137-3226
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Role:
Author
ORCID:
0000-0001-7095-1336
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Publisher:
Springer Nature Publisher's website
Journal:
Nature Chemistry Journal website
Volume:
14
Issue:
1
Pages:
15–24
Publication date:
2021-12-13
Acceptance date:
2021-09-30
DOI:
EISSN:
1755-4349
ISSN:
1755-4330
Pmid:
34903857
Language:
English
Keywords:
Pubs id:
1226046
Local pid:
pubs:1226046
Deposit date:
2021-12-21

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