The DOI matches its Crossref record; 34 of the 34 references it cites were found in a registry or an index.
Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections
Open accessAbstract
Abstract A major resistance mechanism in Gram-negative bacteria is the production of β-lactamase enzymes. Originally recognized for their ability to hydrolyze penicillins, emergent β-lactamases can now confer resistance to other β-lactam drugs, including both cephalosporins and carbapenems. The emergence and global spread of β-lactamase-producing multi-drug-resistant “superbugs” has caused increased alarm within the medical community due to the high mortality rate associated with these difficult-to-treat bacterial infections. To address this unmet medical need, we initiated an iterative program combining medicinal chemistry, structural biology, biochemical testing, and microbiological profiling to identify broad-spectrum inhibitors of both serine- and metallo-β-lactamase enzymes. Lead optimization, beginning with narrower-spectrum, weakly active compounds, provided 20 (VNRX-5133, taniborbactam), a boronic-acid-containing pan-spectrum β-lactamase inhibitor. In vitro and in vivo studies demonstrated that 20 restored the activity of β-lactam antibiotics against carbapenem-resistant Pseudomonas aeruginosa and carbapenem-resistant Enterobacteriaceae. Taniborbactam is the first pan-spectrum β-lactamase inhibitor to enter clinical development.
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Critical analysis of antibacterial agents in clinical development
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Design and discovery of boronic acid drugs
Plescia, J., & Moitessier, N. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112270 · Cited by 201
Metadata
- Authors
- Liu, B., Trout, R. E. L., Chu, G.-H., McGarry, D., Jackson, R. W., Hamrick, J. C., Daigle, D. M., Cusick, S. M., Pozzi, C., De Luca, F., Benvenuti, M., Mangani, S., Docquier, J.-D., Weiss, W. J., Pevear, D. C., Xerri, L., & Burns, C. J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2019-11-25
- Volume
- 63
- Issue
- 6
- Pages
- 2789-2801
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2990621521
- Cited by
- 312
- References
- 34
- FWCI
- 9.64
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Liu, B., Trout, R. E. L., Chu, G.-H., McGarry, D., Jackson, R. W., Hamrick, J. C., Daigle, D. M., Cusick, S. M., Pozzi, C., De Luca, F., Benvenuti, M., Mangani, S., Docquier, J.-D., Weiss, W. J., Pevear, D. C., Xerri, L., & Burns, C. J. (2020). Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.9b01518
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
