The Small Molecules Targeting Ubiquitin-Proteasome System for Cancer Therapy
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
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
Keywords: Ubiquitin, cancer, small molecule inhibitors, proteasome, E3 ligase, deubiquitinating enzyme.
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