GSK2643943A

Description: GSK2643943A is a novel and potent inhibitor of deubiquitylating enzyme (DUB) with an IC50 of 160 nM for USP20/Ub-Rho. The ubiquitin proteasome system is involved in a myriad of biological functions including cell cycle progression, intracellular signaling and protein degradation. As such, it is not surprising to find many components of the system misregulated in cancer. The clinical success of Bortezomib for treatment of multiple myeloma proves that targeting the ubiquitin proteasome system is valid and feasible. Here, a detailed examination of the strategies used to target the ubiquitin proteasome system in cancer is discussed.

References: Nat Rev Drug Discov. 2018 Jan; 17(1):57-78.