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ProteomicsProteomic Ligandability Maps of Phosphorus(V) Stereoprobes Identify Covalent TLCD1 Inhibitors
Activity-based protein profiling (ABPP) of stereoisomerically defined sets of electrophilic compounds (‘stereoprobes’) offers a versatile way to discover covalent ligands for proteins in native biological systems. Here we report the synthesis and chemical proteomic characterization of stereoprobes b...
ORGANISM(S): Homo sapiens (Human) 
2026-09-14 | PXD060339 | Pride
Lipid biology Chemical biology Chemical proteomics Electrophilic probes 
ProteomicsGlobal profiling of phosphorylation-dependent changes in cysteine reactivity
Proteomics has revealed that the ~20,000 human genes engender a far greater number of proteins, or proteoforms, that are diversified in large part by post-translational modifications (PTMs). How such PTMs affect protein structure and function is an active area of research but remains technically cha...
ORGANISM(S): Homo sapiens (Human) 
2022-03-03 | PXD026730 | Pride
Cysteine Activity-based protein profiling Tmt-abpp Mitosis Chemical proteomics Phosphorylation 
ProteomicsExpedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs
A fundamental challenge in chemical biology and medicine is to understand and expand the fraction of the human proteome that can be targeted by small molecules. We recently described a strategy that integrates fragment-based ligand discovery with chemical proteomics to furnish global portraits of re...
ORGANISM(S): Homo sapiens (Human) 
2019-10-29 | PXD015104 | Pride
Human Pbmcs Hek293t Lc-ms/ms 
ProteomicsRemodeling of oncogenic transcriptomes by small molecules targeting the RNA-binding protein NONO
A large swath of the human proteome is dedicated to mRNA homeostasis, but most RNA-binding proteins lack chemical probes1,2. Here, we report the discovery through phenotypic screening of electrophilic small molecules that swiftly (within 4 h) and stereospecifically decrease transcripts encoding the ...
ORGANISM(S): Homo sapiens (Human) 
2024-01-26 | PXD032087 | Pride
Human Lc-msms Tmt Cancer Chemoproteomics Thermo fusion 
ProteomicsA Proteome-Wide Atlas of Lysine-Reactive Chemistry
Recent advances in chemical proteomics have begun to characterize the reactivity and ligandability of lysines on a global scale. Yet, only a limited diversity of aminophilic electrophiles have been evaluated for interactions with the lysine proteome. Here, we report an in-depth profiling of >30 unch...
ORGANISM(S): Homo sapiens (Human) 
2021-09-20 | PXD025829 | Pride
Human immune cells Lysine reactive probes 
ProteomicsStructural and mechanistic analysis of covalent ligands targeting the RNA-binding protein NONO
RNA-binding proteins (RBPs) play important roles in mRNA transcription, processing, and translation. Chemical tools are lacking for RBPs, which has hindered efforts to perturb and understand RBP function in cells. We recently reported a chloroacetamide compound (R)-SKBG-1 that covalently binds the ...
ORGANISM(S): Homo sapiens (Human) 
2026-02-23 | PXD064685 | Pride
Proteomics Chemical biology Rbps Rna-binding protein 
ProteomicsA competitive activity-based protein profiling platform yields cell wall synthesis inhibitors active against replicating and non-replicating Mycobacterium tuberculosis
The identification and validation of a small molecule's targets is a major bottleneck in the discovery process for tuberculosis antibiotics. Activity-based protein profiling (ABPP) is an efficient tool for determining a small molecul's targets within complex proteomes. However, how target inhibition...
ORGANISM(S): Mycobacterium tuberculosis H37Rv 
2022-06-09 | PXD026213 | Pride
Abpp Drug discovery Mycobacterium tuberculosis 
ProteomicsIntegrated phenotypic screening and chemical proteomics identifies ETF1 ligands that modulate viral translation and replication
Emerging and re-emerging viruses pose a significant threat to global health. Although direct-acting antivirals have shown success, their efficacy is limited by the rapid emergence of drug-resistant viral variants. Hence, there is an urgent need for additional broad spectrum antiviral therapeutic str...
ORGANISM(S): Severe acute respiratory syndrome coronavirus 2 Homo sapiens (Human) Alphavirus Influenza A virus Mammarenavirus 
2026-01-29 | PXD067975 | Pride
Ribosomal frameshifting Photo-stereoprobes Activity-based profiling Virus Sars-cov-2 
ProteomicsSelective inhibitors of SARM1 targeting an allosteric cysteine in the autoregulatory ARM domain
The NAD hydrolase (NADase) SARM1 acts as a central executioner of programmed axon death and is a possible therapeutic target for neurodegenerative disorders. While orthosteric inhibitors of SARM1 have been described, this multi-domain enzyme is also subject to intricate forms of autoregulation, sugg...
ORGANISM(S): Homo sapiens (Human) 
2022-08-22 | PXD035400 | Pride
Covalent Chemical proteomics Allosteric inhibition Axonopathy Neurodegeneration 
ProteomicsProteome-wide map of targets of T790M-EGFR-directed covalent inhibitors
Idnetification of the off-targets of several third generation T790M specific inhibtors.
ORGANISM(S): Homo sapiens (Human) Mus musculus (Mouse) 
2019-11-11 | PXD007163 | Pride
Abpp H1975 Co1686 T790m Azd9291 
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