The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Development of the Proteasome Inhibitor Velcade™ (Bortezomib)
Abstract
The dipeptide boronic acid analogue VELCADE (Bortezomib; formerly known as PS-341, LDP-341 and MLM341) is a potent and selective inhibitor of the proteasome, a multicatalytic enzyme that mediates many cellular regulatory signals by degrading regulatory proteins or their inhibitors. The proteasome is, thus, a potential target for pharmacological agents. Bortezomib, the first proteasome inhibitor to reach clinical trials, has shown in vitro and in vivo activity against a variety of malignancies, including myeloma, chronic lymphocytic leukemia, prostate cancer, pancreatic cancer, and colon cancer. The drug is rapidly cleared from the vascular compartment, but a novel pharmacodynamic assay has shown that bortezomib--mediated proteasome blockade is dose-dependent and reversible. Based on phase I studies demonstrating that bortezomib has manageable toxicities in patients with advanced cancers, phase II trials have been initiated for both solid and hematological malignancies.
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Cites
How Proteolysis Drives the Cell Cycle
King, R. W., Deshaies, R. J., Peters, J.-M., & Kirschner, M. W. (1996) · Science · doi:10.1126/science.274.5293.1652 · Cited by 1,273
Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids
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. (1998) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(98)00029-8 · Cited by 685
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Cited by
Inflammation meets cancer, with NF-κB as the matchmaker
Ben-Neriah, Y., & Karin, M. (2011) · Nature Immunology · doi:10.1038/ni.2060 · Cited by 1,373
Deregulated proteolysis by the F-box proteins SKP2 and β-TrCP: tipping the scales of cancer
Frescas, D., & Pagano, M. (2008) · Nature Reviews Cancer · doi:10.1038/nrc2396 · Cited by 890
Kim, Y.-R., Lee, E.-J., Shin, K.-O., Kim, M. H., Pewzner-Jung, Y., Lee, Y.-M., Park, J.-W., Futerman, A. H., & Park, W.-J. (2019) · Experimental & Molecular Medicine · doi:10.1038/s12276-019-0340-1 · Cited by 474
Ubiquitylation in apoptosis: a post-translational modification at the edge of life and death
Vucic, D., Dixit, V. M., & Wertz, I. E. (2011) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm3143 · Cited by 444
Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics
Yang, Y., Kitagaki, J., Dai, R.-M., Tsai, Y. C., Lorick, K. L., Ludwig, R. L., Pierre, S. A., Jensen, J. P., Davydov, I. V., Oberoi, P., et al. (2007) · Cancer Research · doi:10.1158/0008-5472.can-07-0568 · Cited by 441
Metadata
- Authors
- Adams, J., & Kauffman, M.
- Venue
- Cancer Investigation
- Publisher
- Informa UK Limited
- Published
- 2004-01
- Volume
- 22
- Issue
- 2
- Pages
- 304-311
- ISSN
- 0735-7907 (ISSN-L)
- 1532-4192
- OpenAlex
- W2152091753
- Cited by
- 654
- References
- 2
- FWCI
- 9.07
- Type
- journal article
- Language
- en
- Open access
- closed
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