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The Small Molecules Targeting Ubiquitin-Proteasome System for Cancer Therapy

Author(s):

Nannan Ao, Qianping Chen and Geng Liu   Pages 1 - 11 ( 11 )

Abstract:


The ubiquitin-proteasome system (UPS) is responsible for the degradation of majority of the intracellular proteins. The fundamental importance of UPS was highlighted when Rose, Hershko, and Ciechanover were awarded the 2004 Nobel Prize in Chemistry. The alterations in this process have been shown to contribute to the cancer progression. Therefore, pharmacological targeting of the UPS can potentially provide chemotherapeutics for the treatment of tumours. The application of bortezomib proved that interfering with UPS activity could be very effective against haematological malignancies. 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. In this review, we present the crucial components involved in the ubiquitin-proteasome pathway and discuss the current state of small molecules targeting various elements of ubiquitination in cancer treatment.

Keywords:

ubiquitin, cancer, small molecule inhibitors, proteasome, E3 ligase, deubiquitinating enzyme

Affiliation:

School of Radiation Medicine and Protection, Medical College of Soochow University, School for Radiological and Interdisciplinary Sciences (RAD-X), Soochow University, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education In, School of Radiation Medicine and Protection, Medical College of Soochow University, School for Radiological and Interdisciplinary Sciences (RAD-X), Soochow University, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education In, School of Radiation Medicine and Protection, Medical College of Soochow University, School for Radiological and Interdisciplinary Sciences (RAD-X), Soochow University, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education In



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