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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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GARDNER, R. C., Assinder, S. J., Christie, G., MASON, G. G. F., Markwell, R. E., Wadsworth, H., MCLAUGHLIN, M., King, R. J., Chabot‐Fletcher, M., Breton, J., et al. (2000) · Biochemical Journal · doi:10.1042/bj3460447 · Cited by 58
Piperlongumine induces inhibition of the ubiquitin–proteasome system in cancer cells
Jarvius, M., Fryknäs, M., D’Arcy, P., Sun, C., Rickardson, L., Gullbo, J., Haglund, C., Nygren, P., Linder, S. T., & Larsson, R. L. (2013) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2013.01.017 · Cited by 57
Metal-Catalyzed Hydroboration and Diboration of Thiocarbonyls and Vinyl Sulfides
Carter, C. A. G., Vogels, C. M., Harrison, D. J., Gagnon, M.-H., Norman, D. W., Langler, R. F., Baker, R. T. K., & Westcott, S. A. (2001) · Organometallics · doi:10.1021/om010135t · Cited by 57
One-shot NMR analysis of microbial secretions identifies highly potent proteasome inhibitor
Stein, M., Beck, P., Kaiser, M., Dudler, R., Becker, C. F. W., & Groll, M. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1211423109 · Cited by 57
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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