The small molecules targeting ubiquitin-proteasome system for cancer therapy.

The small molecules targeting ubiquitin-proteasome system for cancer therapy.
Comb Chem High Throughput Screen. 2017 Jul 10;:
Authors: Ao N, Chen Q, Liu G
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.
PMID: 28699494 [PubMed - as supplied by publisher]

Source: Combinatorial Chemistry and High Throughput Screening - July 10, 2017 Category: Chemistry Authors: Ao N, Chen Q, Liu G Tags: Comb Chem High Throughput Screen Source Type: research