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ProteomicsDiscovery of a potent and selective covalent inhibitor and activity-based probe for UCHL1, with anti-fibrotic activity
Ubiquitin carboxy-terminal hydrolase L1 (UCHL1) is a deubiquitinating enzyme (DUB) that is very highly expressed in human brain. UCHL1 has been proposed as a potential therapeutic target in neurodegeneration, cancer, and liver and lung fibrosis, however bona fide molecular functions of UCHL1 are yet...
ORGANISM(S): Homo sapiens (Human) 
2020-11-12 | PXD015825 | Pride
Activity based-probe profiling Human Uchl1 Chemical proteomics Deubiquitination 
ProteomicsThioamide-warheads with enhanced cysteine reactivity and specificity for targeted covalent inhibitors
Targeted covalent inhibitors (TCIs) form covalent bond with their target that requires tailored reactive functionalities identified as warheads. Here we present a versatile approach changing carboxamide functions with thioamides that transforms known warheads to softer electrophiles enhancing reacti...
ORGANISM(S): Homo sapiens (Human) 
2026-09-07 | PXD054470 | Pride
Warhead Proteomics Cystein Covalent inhibitors 
ProteomicsElectrophile scanning by chemical prote-omics reveals a potent pan-active DUB probe for investigation of deubiquitinase activity in live cells
Deubiquitinases (DUBs) are proteases that hydrolyze isopeptide bonds linking ubiquitin to protein substrates, which can lead to reduced substrate degradation through the ubiquitin proteasome system. Deregulation of DUB activity has been im-plicated in many disease states, including cancer, neurodege...
ORGANISM(S): Homo sapiens (Human) 
2024-01-03 | PXD035417 | Pride
Ubiquitin-activity base probe Deubiquitinase Chemical probe Activity-based probe Electrophilic war-head Ubiquitin Dub Enzyme targeting Myc-deregulated cancer 
UnknownReactive chemistry for covalent probe and therapeutic development.
Not available
S-EPMC8840975 | biostudies-literature
ProteomicsProteomic analysis of linear ubiquitination substrates based on NAEK-Ub probe in live cells
While linear ubiquitin plays critical roles in multiple cell signaling pathways, few substrates have been identified. Global profiling of linear ubiquitin substrates represents a significant challenge because of the low endogenous level of linear ubiquitination, the none-specific binding of linear p...
ORGANISM(S): Homo Sapiens 
2022-02-11 | PXD031600 |
ProteomicsA chemical probe to monitor parkinsonism-associated protein DJ-1 in live cells
Oxidative stress is a contingent trigger of Parkinson`s disease (PD). DJ-1, a protein involved in oxidative stress sensing, gained major attention when mutations in its gene were identified in PD patients. Although the study of the corresponding protein function is still in its infancy, a crucial ox...
ORGANISM(S): Homo sapiens (Human) 
2018-07-17 | PXD009444 | Pride
Human Lc-ms/ms 
ProteomicsDiscovery of novel covalent ligands with AlphaFold3
Covalent inhibitors are a prominent modality for research and therapeutic tools. However, a scarcity of computational methods for their discovery slows progress in this field. AI models such as AlphaFold3 (AF3) have shown accuracy in ligand pose prediction, but their applicability for virtual screen...
ORGANISM(S): Homo sapiens (Human) 
2026-04-06 | PXD072258 | Pride
Btk Alphafold 
ProteomicsDevelopment of covalent probes to capture Legionella pneumophila effector enzymes
Upon infection of host cells Legionella pneumophila releases a multitude of effector enzymes into the hosts cytoplasm that hijack a plethora of cellular activities, including the hosts ubiquitination pathways. Effectors belonging to the SidE-family are involved in non-canonical serine phosphoribosyl...
ORGANISM(S): Homo sapiens (Human) Legionella pneumophila subsp. pneumophila Lp02 
2025-05-06 | PXD049797 | Pride
Legionella pneumophila Activity-based probe Ubiquitylation Adp-ribosylation Bacterial infection 
ProteomicsTargeted Protein Localization by Covalent 14-3-3 Recruitment
chemoproteomic profiling of covalent ligands that target 14-3-3
ORGANISM(S): Homo sapiens (Human) Mus musculus (Mouse) 
2024-08-28 | PXD054696 | Pride
14-3-3 
GenomicsCovalent Targeting of Splicing in T Cells
Covalent Targeting of Splicing in T Cells
PRJNA1171002 | ENA
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