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Updated: Jun 8, 2026

Cellular Redox Profiling Using High-content Microscopy
Published on: May 14, 2017
[Proteasome inhibitors]
Yasushi Saeki1, Keisuke Fukunaga, Keiji Tanaka
1Laboratory of Protein Metabolism, Tokyo Metropolitan Institute of Medical Science.
Abstract:
The 26S proteasome is a multicatalytic enzyme responsible for degradation of a large fraction of intracellular proteins. Targeting the proteasome activity is a rational and novel strategy for cancer therapy that can lead to cell death for transformed cells. Today, bortezomib, a first-in-class proteasome inhibitor, has established clinical efficacy and an approved clinical indication for the treatment of relapsed and refractory multiple myeloma. Since bortezomib has also shown to induce chemosensitization, the drug is utilized for combination with a variety of chemotherapeutics. In this review, we provide an overview of the current state of the use of bortezomib and second generation proteasome inhibitors.
Insights
The 26S proteasome is a key target for cancer therapy. This review covers bortezomib and newer proteasome inhibitors for treating multiple myeloma and other cancers.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Context:
- The 26S proteasome regulates intracellular protein degradation.
- Targeting proteasome activity offers a novel cancer therapeutic strategy.
- Bortezomib, a proteasome inhibitor, is approved for multiple myeloma.
Purpose:
- To review the clinical applications of bortezomib.
- To discuss the role of proteasome inhibitors in cancer therapy.
- To provide an overview of second-generation proteasome inhibitors.
Summary:
- Bortezomib is a clinically effective proteasome inhibitor for multiple myeloma.
- Proteasome inhibition induces cancer cell death and chemosensitization.
- This review examines current bortezomib use and emerging proteasome inhibitors.
Impact:
- Highlights the therapeutic potential of proteasome inhibition in oncology.
- Informs clinical practice regarding bortezomib and combination therapies.
- Guides future research in the development of novel proteasome inhibitors.
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