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ProteomicsDual-Probe Activity-Based Protein Profiling Reveals Site-Specific Binding Dynamics of EGFR-Directed Drugs
Comparative, dose-dependent analysis of interactions between small molecule drugs and their targets, as well as off-targets, in complex proteomes is crucial for selecting optimal drug candidates. The affinity of small molecules for targeted proteins is largely dictated by interactions between amino ...
ORGANISM(S): Homo sapiens (Human) 
2024-10-17 | PXD045864 | Pride
Chemical proteomics  activity-based protein profiling  site-specific  concentration-dependent analysis  dual-probe comparison. 
ProteomicsValidation and application of a novel KLK6 activity based probe (IMP2352)
Pancreatic cancer has the lowest survival rate of all common cancers due to late diagnosis and limited treatment options. Serine hydrolases are known to mediate cancer progression and metastasis through initiation of signaling cascades and cleavage of extracellular matrix proteins, and the kallikrei...
ORGANISM(S): Homo sapiens (Human) 
2023-03-10 | PXD035111 | Pride
Abpp Klk Activity-based probe Kallikrein-related peptidase N-terminomics 
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 
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 
ProteomicsProtease activity profiling of ovarian clear cell carcinoma
Ovarian clear cell carcinoma (OCCC) is an understudied poor prognosis subtype of ovarian cancer lacking in effective molecularly targeted therapies; efforts to define drivers of OCCC malignancy may lead to new therapeutic targets and approaches. Among potential targets are secreted proteases, enzyme...
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2021-05-07 | MSV000087385 | MassIVE
ProteomicsSITE-SPECIFIC ACTIVITY-BASED PROTEIN PROFILING USING PHOSPHONATE HANDLES
Most drug molecules target proteins. Identification of the exact drug binding sites on these proteins is essential to understand and predict how drugs affect protein structure and function. To address this challenge, we developed a strategy that uses IMAC-enrichable phosphonate affinity tags, for ef...
ORGANISM(S): Homo sapiens (Human) 
2023-01-10 | PXD036569 | Pride
Chemical proteomics  activity-based protein profiling  site-specific  phosphonate affinity handles  fe(iii)-immobilized metal affinity chromatography. 
ProteomicsSmall-Molecule Activity-Based Probe for Monitoring Ubiquitin 2 C‑Terminal Hydrolase (UCHL1) Activity in Live Cells and Zebrafish 3 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 the function of individual enzymes in their native cellular context. Here we report the development of a target-select...
ORGANISM(S): Homo sapiens (Human) 
2020-09-18 | PXD021557 | Pride
Orbitrap Human 
ProteomicsSite-specific Profiling of Lysine Itaconylation via a Thiol-based Probe
Lysine itaconylation is a novel post-translational modification (PTM) that was recently discovered in macrophage proteomes mediated by the immunoregulatory metabolite, itaconate. However, there is currently an absence of comprehensive and high-accuracy analytical methods for the global identificatio...
ORGANISM(S): Mus Musculus Bos Taurus 
2026-04-21 | PXD077428 |
ProteomicsActivity-Based Protein Profiling in Methicillin-Resistant Staphylococcus aureus Reveals Broad Reactivity of a Carmofur-Derived Probe
Activity-based protein profiling is a powerful chemoproteomic technique to detect active enzymes and identify targets and off-targets of drugs. Here, we report on the use of a carmofur-based activity-based probe to identify biologically relevant enzymes in the bacterial pathogen Staphylococcus aureu...
ORGANISM(S): Bacteria Staphylococcus aureus 
2024-01-29 | PXD043275 | Pride
Biofilm Activity-based protein profiling Carmofur S. aureus 
ProteomicsCIMAGE2.0: An Expanded Tool for Quantitative Analysis of Activity-based Probe Profiling (ABPP) Data
Activity-based Protein Profiling (ABPP) is a powerful chemo-proteomic method to study proteins’ activity, modifications and interactions in a high-throughput manner. In ABPP experiments, accurate quantification is crucial to determine the extent of probe labeling at the level of either target protei...
ORGANISM(S): Homo Sapiens 
2021-03-16 | PXD024754 |
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