The proteasome, a new target for cancer therapy
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Updated: Sep 21, 2026

Quantitative Mass Spectrometric Profiling of Cancer-cell Proteomes Derived From Liquid and Solid Tumors
Published on: February 27, 2015
S Gillessen1, M Groettup, T Cerny
1Department of Oncology/Hematology, Kantonsspital St. Gallen, Switzerland. silke.gillessen@kssg.ch
Abstract:
The proteasome is a multicatalytic protease and the principal non-lysosomal proteolytic system in all eukaryotic cells. It plays a central role in virtually all regulatory pathways as for instance cell-cycle regulation, differentiation, and apoptosis. The proteasome degrades regulatory proteins and their inhibitors and, thus is an interesting target for therapeutic drugs. Inhibitors of the proteasome are small molecules that function by stabilizing various proteins, including cell-cycle regulators, tumor suppressors and growth factors. Because proteasome inhibition blocks cellular proliferation and induces apoptosis, these agents have been tested as anticancer drugs in tumor models and have shown impressive potential. In addition, treatment with proteasome inhibitors can sensitize cells to other cancer treatments like radio- or chemotherapy. This review introduces the ubiquitin-proteasome pathway and outlines the recent progress in the development of proteasome inhibition as a treatment option for clinical cancer therapy.
Insights
The proteasome is a key cellular machine that degrades proteins. Proteasome inhibitors show promise as anticancer drugs by blocking cell proliferation and inducing apoptosis.
Area of Science:
- Biochemistry
- Molecular Biology
- Cell Biology
Background:
- The proteasome is a crucial proteolytic system in eukaryotic cells.
- It regulates key cellular processes like cell-cycle control, differentiation, and apoptosis.
- Dysregulation of proteasome function is implicated in various diseases, including cancer.
Purpose of the Study:
- To review the ubiquitin-proteasome pathway.
- To outline recent advancements in proteasome inhibition for cancer therapy.
Main Methods:
- This review synthesizes current research on the proteasome and its inhibitors.
- It discusses the mechanism of action of proteasome inhibitors.
- It examines their therapeutic potential in preclinical cancer models.
Main Results:
- Proteasome inhibitors stabilize regulatory proteins, blocking cell proliferation.
- These inhibitors induce apoptosis, a key mechanism in cancer cell death.
- Proteasome inhibition can enhance sensitivity to conventional cancer treatments.
Conclusions:
- Proteasome inhibition is a promising therapeutic strategy for cancer.
- Further development of proteasome inhibitors holds significant clinical potential.
- The ubiquitin-proteasome pathway remains an important target for drug discovery.
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