Recent advances in activity-based probes (ABPs) and affinity-based probes (A f BPs) for profiling of enzymes
Activity-based protein profiling (ABPP) is a technique that uses highly selective active-site
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …
Accelerating inhibitor discovery for deubiquitinating enzymes
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 …
cleave ubiquitin from protein substrates to regulate many cellular processes. A lack of …
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 …
ubiquitination dynamics. Since their discovery, genetic and functional studies have …
Native semisynthesis of isopeptide-linked substrates for specificity analysis of deubiquitinases and Ubl proteases
Post-translational modifications with ubiquitin (Ub) and ubiquitin-like proteins (Ubls) are
regulated by isopeptidases termed deubiquitinases (DUBs) and Ubl proteases. Here, we …
regulated by isopeptidases termed deubiquitinases (DUBs) and Ubl proteases. Here, we …
Discovery of a Potent Deubiquitinase (DUB) Small‐Molecule Activity‐Based Probe Enables Broad Spectrum DUB Activity Profiling in Living Cells
Deubiquitinases (DUBs) are a family of> 100 proteases that hydrolyze isopeptide bonds
linking ubiquitin to protein substrates, often leading to reduced substrate degradation …
linking ubiquitin to protein substrates, often leading to reduced substrate degradation …
Activity‐based probes for the ubiquitin conjugation–deconjugation machinery: new chemistries, new tools, and new insights
DS Hewings, JA Flygare, M Bogyo… - The FEBS journal, 2017 - Wiley Online Library
The reversible post‐translational modification of proteins by ubiquitin and ubiquitin‐like
proteins regulates almost all cellular processes, by affecting protein degradation …
proteins regulates almost all cellular processes, by affecting protein degradation …
Small-molecule activity-based probe for monitoring ubiquitin C-terminal hydrolase L1 (UCHL1) activity in live cells and zebrafish embryos
Many reagents have emerged to study the function of specific enzymes in vitro. On the other
hand, target specific reagents are scarce or need improvement, allowing investigations of …
hand, target specific reagents are scarce or need improvement, allowing investigations of …
Discovery of a potent and selective covalent inhibitor and activity-based probe for the deubiquitylating enzyme UCHL1, with antifibrotic activity
Ubiquitin carboxy-terminal hydrolase L1 (UCHL1) is a deubiquitylating enzyme that is
proposed as a potential therapeutic target in neurodegeneration, cancer, and liver and lung …
proposed as a potential therapeutic target in neurodegeneration, cancer, and liver and lung …
Cell-permeable activity-based ubiquitin probes enable intracellular profiling of human deubiquitinases
Advancement in our knowledge of deubiquitinases (DUBs) and their biological functions
requires biochemical tools permitting interrogation of DUB activities under physiologically …
requires biochemical tools permitting interrogation of DUB activities under physiologically …