Advances in discovering deubiquitinating enzyme (DUB) inhibitors

NJ Schauer, RS Magin, X Liu, LM Doherty… - Journal of medicinal …, 2019 - ACS Publications
Deubiquitinating enzymes, or DUBs, comprise a family of proteases that regulate
ubiquitination dynamics. Since their discovery, genetic and functional studies have …

Advances in the development ubiquitin-specific peptidase (USP) inhibitors

S Chen, Y Liu, H Zhou - International journal of molecular sciences, 2021 - mdpi.com
Ubiquitylation and deubiquitylation are reversible protein post-translational modification
(PTM) processes involving the regulation of protein degradation under physiological …

A proteome-scale map of the SARS-CoV-2–human contactome

DK Kim, B Weller, CW Lin, D Sheykhkarimli… - Nature …, 2023 - nature.com
Understanding the mechanisms of coronavirus disease 2019 (COVID-19) disease severity
to efficiently design therapies for emerging virus variants remains an urgent challenge of the …

Accelerating inhibitor discovery for deubiquitinating enzymes

WC Chan, X Liu, RS Magin, NM Girardi… - Nature …, 2023 - nature.com
Deubiquitinating enzymes (DUBs) are an emerging drug target class of~ 100 proteases that
cleave ubiquitin from protein substrates to regulate many cellular processes. A lack of …

USP25 promotes pathological HIF-1-driven metabolic reprogramming and is a potential therapeutic target in pancreatic cancer

JK Nelson, MZ Thin, T Evan, S Howell, M Wu… - Nature …, 2022 - nature.com
Deubiquitylating enzymes (DUBs) play an essential role in targeted protein degradation and
represent an emerging therapeutic paradigm in cancer. However, their therapeutic potential …

From discovery to bedside: targeting the ubiquitin system

IE Wertz, X Wang - Cell chemical biology, 2019 - cell.com
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 …

USP25 inhibition ameliorates Alzheimer's pathology through the regulation of APP processing and Aβ generation

Q Zheng, B Song, G Li, F Cai, M Wu… - The Journal of …, 2022 - Am Soc Clin Investig
Down syndrome (DS), or trisomy 21, is one of the critical risk factors for early-onset
Alzheimer's disease (AD), implicating key roles for chromosome 21–encoded genes in the …

Deubiquitylating enzymes in cancer and immunity

J Ren, P Yu, S Liu, R Li, X Niu, Y Chen… - Advanced …, 2023 - Wiley Online Library
Deubiquitylating enzymes (DUBs) maintain relative homeostasis of the cellular ubiquitome
by removing the post‐translational modification ubiquitin moiety from substrates. Numerous …

Trisomy 21–induced dysregulation of microglial homeostasis in Alzheimer's brains is mediated by USP25

Q Zheng, G Li, S Wang, Y Zhou, K Liu, Y Gao… - Science …, 2021 - science.org
Down syndrome (DS), caused by trisomy of chromosome 21, is the most significant risk
factor for early-onset Alzheimer's disease (AD); however, underlying mechanisms linking DS …

Regulation of cancer metabolism by deubiquitinating enzymes: the Warburg effect

SH Kim, KH Baek - International Journal of Molecular Sciences, 2021 - mdpi.com
Cancer is a disorder of cell growth and proliferation, characterized by different metabolic
pathways within normal cells. The Warburg effect is a major metabolic process in cancer …