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ProteomicsQuantitative Chemical Proteomic Profiling of Ubiquitin Specific Proteases in Intact Cancer Cells
Deubiquitinating enzymes play an important role in a plethora of therapeutically relevant processes, and are emerging as pioneering drug targets. Herein, we present a novel Ubiquitin Specific Protease (USP) inhibitor, alongside an alkyne-tagged activity-based probe analogue. Activity-based proteome ...
ORGANISM(S): Homo sapiens (Human) 
2016-12-14 | PXD004875 | Pride
Abpp Chemical proteomics Lc-msms Ubiquitin 
ProteomicsDevelopment of Photocrosslinking Probes Based on Huwentoxin-IV to Map the Site of Interaction on Nav1.7
This study reports on the design of a library of photoprobes based on the potent spider toxin Huwentoxin-IV and the determination of the toxin binding interface on VSD2 of Nav1.7 through a photocrosslinking and tandem mass spectrometry approach. Our Huwentoxin-IV probes selectively crosslink to extr...
ORGANISM(S): Homo sapiens (Human) 
2019-11-18 | PXD015037 | Pride
Nav1.7 Photoaffinity labelling Huwentoxin-iv Diazirine Peptide mapping 
ProteomicsIdentification of protein-protein interactions in live cells using photoactivatable myristate probe X10
19 TST-tagged myristoylated proteins (baits) were transfected into cells and labeled with photoactivatable clickable myristate probe X10. mCitrine-TST was used as a negative control. X10-labeled proteins were photocrosslinked in live cells to their interacting partners with the aim of identifying ne...
ORGANISM(S): Homo sapiens (Human) 
2023-02-04 | PXD027394 | Pride
Myristoylation  photocrosslinking  protein-protein interaction 
ProteomicsChemical proteomics identifies a novel off-target protein of small molecule NLRP3 inflammasome inhibitor MCC950
Inhibition of inflammasome and pyroptotic pathways are promising strategies for clinical treatment of autoimmune and inflammatory disorders. MCC950, a potent inhibitor of the NLR-family inflammasome pyrin domain-containing 3 (NLRP3) protein, has shown encouraging results in animal models for a range...
ORGANISM(S): Homo sapiens (Human) 
2021-05-17 | PXD024915 | Pride
Human Mcc950 Thp1 Lc-ms/ms 
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 
ProteomicsQuantitative chemical proteomic analysis of YnMyr-tagged proteins in HeLa cells infected with RV16
Rhinovirus causes the common cold and drives exacerbation in asthma and COPD, leading to substantial morbidity and healthcare cost. The single positive strand RNA genome of this non-enveloped virus is translated into a single polyprotein that is processed by virus 3C protease to form three structura...
ORGANISM(S): Homo sapiens (Human) 
2018-05-09 | PXD005798 | Pride
Hela Rv16 Proteomics Myristoylation Nmt inhibition 
ProteomicsCompetition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane
Sulforaphane is a small molecule isothiocyanate which exhibits anticancer potential, yet its biological targets remain poorly understood. Here we employ a competition-based chemical proteomics strategy to profile sulforaphane’s targets and identify over 500 targets along with their relative affiniti...
ORGANISM(S): Homo sapiens (Human) 
2017-05-24 | PXD006279 | Pride
Sulforaphane  cancer  chemical proteomics 
Proteomicshuman LHR-APEX2 time-resolved proximity proteomics
Cellular signaling by membrane G protein-coupled receptors (GPCRs) is orchestrated by a complex and diverse array of mechanisms. The dynamics of a GPCR interactome as it evolves over time and space in response to an agonist can offer a unique window on pleiotropic signaling decoding and functional s...
ORGANISM(S): Homo sapiens (Human) 
2026-03-20 | PXD053246 | Pride
Proteomics Proximity proteomics Apex2 Lhcgr Lhr Interactomics Gpcr Human 
ProteomicsRe-evaluation of the mechanism of action of α,β-unsaturated carbonyl DUB inhibitors b-AP15 and VLX1570: CIAPIN1 is a major target of VLX1570 for non-selective covalent modification and aggregation in a multiple myeloma model.
Deubiquitinating enzymes are a growing target class across multiple disease states, with several inhibitors now reported. b-AP15 and VLX1570 are two structurally related USP14/UCH-37 inhibitors. Initially taken forward into a phase I/II clinical trial for refractory Multiple Myeloma, VLX1570 has sin...
ORGANISM(S): Homo sapiens (Human) 
2020-05-26 | PXD015412 | Pride
Proteomics Vlx1570 Chemoproteomics Bap-15 Multiple myeloma 
UnknownReconstructing evolutionary trajectories of mutation signature activities in cancer using TrackSig.
Not available
S-EPMC7002414 | biostudies-literature
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