Deubiquitinase-targeting chimeras for targeted protein stabilization
NJ Henning, L Boike, JN Spradlin, CC Ward… - Nature chemical …, 2022 - nature.com
Many diseases are driven by proteins that are aberrantly ubiquitinated and degraded. These
diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we …
diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we …
[HTML][HTML] Applications of protein ubiquitylation and deubiquitylation in drug discovery
Y Chen, H Xue, J Jin - Journal of Biological Chemistry, 2024 - Elsevier
The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …
Reversible assembly of proteolysis targeting chimeras
PROteolysis TArgeting Chimeras (PROTACs) are of significant current interest for the
development of probe molecules and drug leads. However, they suffer from certain …
development of probe molecules and drug leads. However, they suffer from certain …
Protein degradation by in-cell self-assembly of proteolysis targeting chimeras
H Lebraud, DJ Wright, CN Johnson… - ACS central …, 2016 - ACS Publications
Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a
promising potential alternative to protein inhibition for therapeutic intervention. Current …
promising potential alternative to protein inhibition for therapeutic intervention. Current …
Lessons in PROTAC design from selective degradation with a promiscuous warhead
Inhibiting protein function selectively is a major goal of modern drug discovery. Here, we
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
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 …
Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …
degrading disease-causing proteins. While many PROTACs have been developed for …
Conformational stabilization of ubiquitin yields potent and selective inhibitors of USP7
Y Zhang, L Zhou, L Rouge, AH Phillips, C Lam… - Nature chemical …, 2013 - nature.com
Protein conformation and function are often inextricably linked, such that the states a protein
adopts define its enzymatic activity or its affinity for various partners. Here we combine …
adopts define its enzymatic activity or its affinity for various partners. Here we combine …
Enzyme-catalyzed activation of pro-PROTAC for cell-selective protein degradation
C Liang, Q Zheng, T Luo, W Cai, L Mao… - CCS …, 2022 - chinesechemsoc.org
Proteolysis targeting chimera (PROTAC) technology is a chemical protein knockdown
approach that degrades protein by hijacking the cellular ubiquitin-proteasome system to …
approach that degrades protein by hijacking the cellular ubiquitin-proteasome system to …
Chemical and semisynthetic approaches to study and target deubiquitinases
P Gopinath, S Ohayon, M Nawatha, A Brik - Chemical Society Reviews, 2016 - pubs.rsc.org
Ubiquitination is a key posttranslational modification, which affects numerous biological
processes and is reversed by a class of enzymes known as deubiquitinases (DUBs). This …
processes and is reversed by a class of enzymes known as deubiquitinases (DUBs). This …