Abstract LB-049: Targeting the ubiquitin-proteasome system by small molecule inhibition of the DUBome

Abstract:

The current interest in protein homeostasis as a therapeutic strategy has highlighted the importance of protein ubiquitination as a post-translational modification. Protein degradation has been enabled by several approaches (e.g. small molecule degraders, molecular glues, and PROTACsTM). Deubiquitinating enzymes (DUBs) are proteases that catalyse the de-ubiquitination of protein substrates and as such offer an alternative way to regulate protein homeostasis. Furthermore, since ubiquitination also controls a plethora of regulatory functions beyond direct degradation, inhibition of DUBs provides additional opportunities to manipulate critical cellular processes. As a result of this dual role in protein degradation and signalling, as well as their increasing linkage to the etiology of numerous pathological conditions including cancer and neurodegeneration, DUBs have emerged as an attractive target class for the …

Año de publicación:

2019

Keywords:

Fuente:

google