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GenomicsIdentification of covalent small-molecule inhibitors of STING
Identification of covalent small-molecule inhibitors of STING
PRJNA454500 | ENA
ProteomicsLysine-targeting, covalent inhibitors of bromodomain BD1 of BET proteins in live cells and animals
We report herein a set of activity-based probes (ABPs; P3-P7) based on various lysine-reactive covalent warheads capable of global profiling of ligandable lysine within BRDs in live cells and animals. Chemoproteomic experiments with P7 by utilizing 2-ethynylbenzaldehyde (EBA) identified 18 endogenou...
ORGANISM(S): Homo Sapiens Mus Musculus 
2025-04-10 | PXD058513 |
GenomicsDevelopment of potent and selective KDM5 covalent inhibitors
Development of potent and selective KDM5 covalent inhibitors
PRJNA486160 | ENA
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 
ProteomicsHigh-Throughput Screening of Amyloid Inhibitors via Covalent-Labeling Mass Spectrometry
MS spectra of DEPC modifications on beta-2-microglobulin (b2m) residues under amyloid-forming conditions, with or without 4-hydroxythalidomide.
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2025-06-25 | MSV000098322 | MassIVE
TranscriptomicsIdentification of covalent small-molecule inhibitors of STING
Identification of covalent small-molecule inhibitors of STING
ORGANISM(S): Mus musculus 
2018-05-02 | GSE113933 | GEO
ProteomicsMapping in vivo target interaction profiles of covalent inhibitors using chemical proteomics with label-free quantification
Activity-based protein profiling (ABPP) has emerged as a valuable chemical proteomics method to guide the therapeutic development of covalent drugs by assessing their on-target engagement and off-target activity. Recently, we reported on the establishment, by ABPP, of the serine hydrolase interactio...
ORGANISM(S): Mus musculus (Mouse) 
2018-02-23 | PXD007965 | Pride
Activity-based protein profiling  covalent inhibitors  chemical proteomics  label-free quantification  target engagement 
ProteomicsOn-board Preconcentration Microchip Capillary Electrophoresis Based TMT-PRM-LIVE for High-throughput Selectivity Profiling of Deubiquitinase Inhibitors
On-board Preconcentration Microchip Capillary Electrophoresis Based TMT-PRM-LIVE for High-throughput Selectivity Profiling of Deubiquitinase Inhibitors
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2022-03-24 | MSV000089122 | MassIVE
ProteomicsIdentification of the covalent binding site of Ibrutinib and 5Z-7-Oxozeaenol to ZAK
The goal of this experiment was to identify the reaction site of Ibrutinib and 5Z-7-Oxozeaenol to ZAK by determination of mass shifts according to a covalent modification by the inhibitors using mass spectrometry.
ORGANISM(S): Homo sapiens (Human) 
2017-10-13 | PXD007752 | Pride
Ibrutinib 5z-7-oxozeaenol Cys150 Recombinant zak Cys22 Covalent modification 
GenomicsTargeting transcriptional dependencies in cancer using a covalent CDK7 inhibitor (ChIP-Seq)
Cyclin-dependent kinase 7 (CDK7) plays a critical role in the general regulation of RNA polymerase II-mediated transcription. However, the absence of selective CDK7 inhibitors has hindered the ability to investigate the consequences of acute and prolonged inhibition of CDK7 under normal and patholo...
ORGANISM(S): Homo sapiens 
2013-12-23 | E-GEOD-50622 | biostudies-arrayexpress
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