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Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids
Abstract
Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.
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“Exchange of the aldehyde electrophile for a boronic acid substantially increased the potency of proteasome inhibition121.”
From Advances in covalent drug discovery (2022) · cites this paper as [121]
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Metadata
- Authors
- Adams, J., Behnke, M., Chen, S., Cruickshank, A. A., Dick, L. R., Grenier, L., Klunder, J. M., Ma, Y.-T., Plamondon, L., & Stein, R. L.
- Venue
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier BV
- Published
- 1998-02
- Volume
- 8
- Issue
- 4
- Pages
- 333-338
- ISSN
- 0960-894X (ISSN-L)
- OpenAlex
- W1992978957
- Cited by
- 685
- References
- 20
- Citations by year
- 2026: 7 · 2025: 9 · 2024: 15 · 2023: 12 · 2022: 15 · 2021: 32 · 2020: 20 · 2019: 23 · 2018: 25 · 2017: 17 · 2016: 25 · 2015: 21 · 2014: 42 · 2013: 25 · 2012: 39
- FWCI
- 5.01
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Bioorganic & Medicinal Chemistry Letters (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Protease and Inhibitor Mechanisms
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Keywords
- proteasome inhibitors, boronic acid, selective inhibitors, cancer therapeutics, inflammatory diseases
- MeSH terms
- Boronic Acids, Cysteine Endopeptidases, Multienzyme Complexes, Protease Inhibitors, Molecular Structure, Proteasome Endopeptidase Complex
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