From Discovery to Bedside: Targeting the Ubiquitin System. Issue 2 (21st February 2019)

• Record Type: Journal Article
• Authors: Wertz, Ingrid E.; Wang, Xiaojing
• Is Part Of: Cell chemical biology. Volume 26:Issue 2(2019)
• Page Start: 156
• Page End: 177
• Publication Date: 2019-02-21
• Subjects: ubiquitin -- ubiquitin ligase -- E3 -- deubiquitinase -- DUB -- proteasome -- degradation; Biochemistry -- Periodicals; 572.05
• DOI: 10.1016/j.chembiol.2018.10.022
• Languages: English
• ISSNs: 2451-9456

Abstract

Abstract : The ubiquitin/proteasome system is a primary conduit for selective intracellular protein degradation. Since its discovery over 30 years ago, this highly regulated system continues to be an active research area for drug discovery that is exemplified by several approved drugs. Here we review compounds in preclinical testing, clinical trials, and approved drugs, with the aim of highlighting innovative discoveries and breakthrough therapies that target the ubiquitin system. Abstract : The ubiquitin system is a major regulator of selective intracellular protein degradation and is essential for maintaining homeostasis. Dysregulation is associated with pathogenesis, thus targeting the ubiquitin system is an expanding area in drug discovery. Here, Wertz and Wang review compounds in preclinical studies, clinical trials, and approved therapeutics.