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ProteomicsComprehensive chemical proteomics analyses reveal that the new TRi-1 and TRi-2 compounds are more specific thioredoxin reductase 1 inhibitors than Auranofin
Anticancer drugs that target cellular antioxidant systems have recently attracted much attention. Auranofin (AF) is currently evaluated in several clinical trials as an anticancer agent and targets the cytosolic and mitochondrial forms of the selenoprotein thioredoxin reductase, Txnrd1 and Txnrd2. R...
ORGANISM(S): Mus musculus (Mouse) 
2021-12-15 | PXD028398 | Pride
Inhibition Thioredoxin reductase Cancer Proteomics Mouse 
ProteomicsThermoTargetMiner: Proteome Integral Solubility Alteration (PISA) target database for prospective lung cancer drug candidates
Knowledge of the targets of therapeutic compounds helps understanding the compound action mechanism as well as the side-effects. The multiple complementary techniques needed for comprehensive target characterization must combine data reliability with sufficient analysis throughput. Here, we test the...
ORGANISM(S): Homo sapiens (Human) 
2026-06-08 | PXD054158 | Pride
Human Proteomics Lc-ms Lung cancer 
ProteomicsComprehensive chemical proteomics for target deconvolution of the redox active drug auranofin
Chemical proteomics encompasses novel drug target deconvolution methods in which compound modification is not required. Herein we use Thermal Proteome Profiling, Functional Identification of Target by Expression Proteomics and multiplexed redox proteomics for deconvolution of auranofin targets to ai...
ORGANISM(S): Homo sapiens (Human) 
2020-03-19 | PXD016776 | Pride
Cancer Nfkb2 Mass spectrometry Hct116 Thioredoxin reductase Expression Chordc1 Database A375 Drug Proteomics Resource Rko Chemotherapeutic Auranofin Compound 
ProteomicsIon-based Proteome Integrated Solubility Alteration Assay for System-wide Profiling of Protein-Molecule Interactions - full curve data
Unbiased drug target engagement deconvolution and mechanism of action elucidation are major challenges in drug development. Modification-free target engagement methods, such as thermal proteome profiling, have gained increasing popularity over the last several years. However, these methods have limi...
ORGANISM(S): Homo sapiens (Human) 
2022-06-09 | PXD033081 | Pride
Proteomics Mechanism of action Drug target deconvolution Thermal protein profiling Cancer 
ProteomicsSystem-wide profiling of drug residence time by proteome integral solubility alteration assay
Most drugs used in the clinic and drug candidates target multiple proteins, and thus detailed characterization of their efficacy targets is required. While current methods rely on quantitative measurements at thermodynamic equilibrium, kinetic parameters such as the residence time of a drug on its t...
ORGANISM(S): Homo sapiens (Human) 
2023-01-06 | PXD034351 | Pride
Target engagement Drug development Thermal proteome profiling. Efficacy target Lead compound optimization Target prioritization Binding affinity Precision medicine Target occupancy 
ProteomicsProteomics to determine metallodrug targets and optimal drug combinations
The FITExP profiling approach was used to identify protein hits from cells incubated with RAPTA-T or RAPTA-EA. Validation experiments with paclitaxel and cisplatin underlined the reliability of the method and hit lists for both test compounds (and?) gave physiologically viable anti-cancer mechanisms...
ORGANISM(S): Homo sapiens (Human) 
2018-02-09 | PXD005766 | Pride
Drug targets Fitexp Cancer 
ProteomicsSystem-wide identification of enzyme substrates by thermal analysis (SIESTA)
Despite the immense importance of enzyme-substrate reactions, there is a lack of general and unbiased tools for identifying the molecular components participating in these reactions on a cellular level. Here we developed a universal method called System-wide Identification of Enzyme Substrates by Th...
ORGANISM(S): Homo sapiens (Human) 
2021-01-11 | PXD010554 | Pride
Poly-(adp-ribose) polymerase-10 Post-translational modification Target Thioredoxin reductase 1 Artd10 Thermal stability Trxr1 Parp10 Marylation Substrate 
ProteomicsPolymorphisms of the vitamin D receptor regulate T cells and T cell dependent inflammatory diseases
Complex autoimmune diseases have proven difficult to dissect down to their causative genetic mechanisms. As a result, epidemiological data from different human association studies are often merged to arrive at a working hypothesis. In one of such examples, lack of sun exposure and consequent lower s...
ORGANISM(S): Mus musculus (Mouse) 
2020-09-28 | PXD019876 | Pride
T cell Inflammatory disease Vitamin d3 
ProteomicsProteomics study of THP-1 monocytic cells exposed to surface modified-gold nanoparticles
A proteome comparison was performed to assess the responses of human monocytic cells (THP-1) to gold-nanoparticles (Au-NPs) of two different diameter sizes (5 or 20 nm) with different surface functional groups, i.e., alkylammonium bromide, alkyl sodium carboxylate, or poly(ethylene glycol) (PEG)-ter...
ORGANISM(S): Homo sapiens (Human) 
2019-03-18 | PXD010858 | Pride
Thp-1 monocytes Proteomics Gold-nanoparticles 
ProteomicsHLA-DR peptides from human BAL and EBV-transformed B cells
Optimization of the protocols for isolation HLA-DR (MHCII) peptides from human BAL.
ORGANISM(S): Homo sapiens (Human) 
2016-08-08 | PXD002439 | Pride
Bal Sarcoidosis Hla-dr peptides 
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