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ProteomicsCovalent fragment screening to inhibit the E3 ligase activity of bacterial NEL enzymes SspH1 and SspH2
As the global fight against antimicrobial resistance in bacteria becomes increasingly pressing, new tool compounds are needed to understand and identify novel therapeutic targets. Here, cysteine-directed fragment-based drug discovery is coupled with a high throughput chemistry direct-to-biology scre...
ORGANISM(S): Homo sapiens (Human) 
2025-11-10 | PXD057304 | Pride
Bacterial nels Fragment-based drug discovery Covalent fragments Salmonella effectors Chemoproteomics E3 ligase High throughput chemistry 
ProteomicsProfiling Sulfur(VI) Fluorides as Reactive Functionalities for Chemical Biology Tools and Expansion of the Ligandable Proteome
Here, we profiled sulfur(VI) fluorides (SVI-F) as reactive functionalities that can modify multiple residues including Lys, Tyr, His and Ser, thus offering utility for targeting almost any protein. These studies provided an in-depth understanding of SVI-F functionalities, including hydrolytic stabil...
ORGANISM(S): Homo sapiens (Human) 
2024-03-18 | PXD037048 | Pride
Covalent probes Covalent fragment screening Sulfonyl fluoride Chemical biology 
ProteomicsA chemoproteomic platform for selective deubiquitinase inhibitor discovery
Here we describe our work on the development of an ABPP screening platform for cysteine reactive covalent fragments against deubiquitinating enzymes (DUBs) on 96 well plate format. Within this targeted workflow, we profile cysteine reactive fragments by competition with biotinylated ubiquitin probe ...
ORGANISM(S): Homo sapiens (Human) 
2024-03-18 | PXD037152 | Pride
Dubs Covalent probes Covalent fragment screening Chemical biology Activity-based protein profiling 
ProteomicsA chemoproteomic platform for selective deubiquitinase inhibitor discovery
Here we describe our work on the development of an ABPP screening platform for cysteine reactive covalent fragments against deubiquitinating enzymes (DUBs) on 96 well plate format. Within this targeted workflow, we profile cysteine reactive fragments by competition with biotinylated ubiquitin probe ...
ORGANISM(S): Homo sapiens (Human) 
2024-03-18 | PXD037114 | Pride
Dubs Covalent probes Covalent fragment screening Chemical biology Activity-based protein profiling 
ProteomicsEnantioselective OTUD7B fragment discovery through chemoproteomics screening and high-throughput optimisation
Deubiquitinating enzymes (DUBs) are key regulators of cellular homeostasis, and their dysregulation is associated with several human diseases. The ovarian tumour protease (OTU) family of DUBs are biochemically well-characterised and of therapeutic interest, yet only a few tool compounds exist to stu...
ORGANISM(S): Homo sapiens (Human) 
2025-01-13 | PXD057851 | Pride
Dubs Dia Iodoacetamide-desthiobiotin (ia-dtb) Chemoproteomics Cysteine reactivity profiling Abpp 
ProteomicsEnantioselective OTUD7B fragment discovery through chemoproteomics screening and high-throughput optimisation
Here we present a chemoproteomics fragment screening platform for identifying novel DUB-specific hit matter, that combines activity-based protein profiling with high-throughput chemistry direct-to-biology optimisation to enable rapid elaboration of initial fragment hits against OTU DUBs. Applying th...
ORGANISM(S): Homo sapiens (Human) 
2025-01-13 | PXD054883 | Pride
Chemoproteomics Covalent fragments Data-independent acquisition Activity-based protein profiling Deubiquitinating enzymes 
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