Related Experiment Video
Updated: Feb 26, 2026

Evaluation of Substrate Ubiquitylation by E3 Ubiquitin-ligase in Mammalian Cell Lysates
Published on: May 10, 2022
The Small Molecules Targeting Ubiquitin-Proteasome System for Cancer Therapy
Nannan Ao1, Qianping Chen1, Geng Liu1
1School of Radiation Medicine and Protection, Medical College of Soochow University, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education Institutions, Suzhou 215123. China.
Background & Aim:
The ubiquitin-proteasome system (UPS) is the major pathway for degrading the intracellular proteins. The 2004 Nobel Prize in Chemistry was awarded to Rose, Hershko, and Ciechanover to highlight the fundamental importance of UPS.
Method & Results:
The alterations in this process have been shown to contribute to the cancer progression. Hence, UPS has become a popular target for developing chemotherapeutics against tumours. The application of bortezomib showed high efficiency in treating haematological malignancies by interfering with UPS activity. Many compounds are being screened and evaluated in recent pharmacological advances, either as single agents or in synergy with other drugs, and more to be revealed.
Conclusion:
In the present review, we exhibit the crucial ingredients involved in UPS and discuss the current situation of small molecules targeting various components of ubiquitination pathway in cancer treatment.
Insights
The ubiquitin-proteasome system (UPS) degrades intracellular proteins and is crucial in cancer progression. Targeting UPS with small molecules offers a promising strategy for developing novel cancer therapeutics.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- The ubiquitin-proteasome system (UPS) is a fundamental cellular pathway responsible for intracellular protein degradation.
- Dysregulation of the UPS is implicated in the pathogenesis and progression of various cancers.
Purpose of the Study:
- To review the key components of the UPS.
- To discuss the therapeutic potential of small molecules targeting the ubiquitination pathway in cancer treatment.
Main Methods:
- Literature review of the ubiquitin-proteasome system.
- Analysis of current research on small molecules targeting ubiquitination pathways.
Main Results:
- The UPS plays a critical role in cellular protein homeostasis and is frequently altered in cancer.
- Bortezomib, a UPS inhibitor, has demonstrated efficacy in treating hematological malignancies.
- Numerous compounds are under investigation for their potential in cancer therapy, as single agents or in combination.
Conclusions:
- The UPS is a vital target for anticancer drug development.
- Small molecules modulating ubiquitination pathways represent a significant area of research for novel cancer treatments.
More Related Videos
10:25Screening Traditional Chinese Medicine Compounds for Inhibiting UCHL3 Activity Based on Molecular Docking and Deubiquitinating Enzyme Probe Technology
Published on: November 22, 2024
10:26Profiling Ubiquitin and Ubiquitin-like Dependent Post-translational Modifications and Identification of Significant Alterations
Published on: November 7, 2019
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against...
The Proteasome
In this pathway, the target proteins are first tagged with small proteins called ubiquitin. A series of enzymes carry out the ubiquitination of the target proteins - E1 (ubiquitin-activating enzyme), E2 (ubiquitin-conjugating enzyme), and E3...
The Proteasome
In this pathway, the target proteins are first tagged with small proteins called ubiquitin. This involves participation of a series of enzymes including— E1 (ubiquitin-activating enzyme), E2 (ubiquitin-conjugating enzyme), and E3...
Drugs that Stabilize Microtubules
Drugs that Destabilize Microtubules
Site-Targeted Drug Delivery Systems: Polymeric Carriers