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GenomicsDevelopment of potent and selective KDM5 covalent inhibitors
Development of potent and selective KDM5 covalent inhibitors
PRJNA486160 | ENA
ProteomicsCovalent allosteric inhibition of AARS1 lactyltransferase
Alanyl-tRNA synthetase 1 (AARS1) was recently identified as a lactyltransferase responsible for protein lactylation, a modification associated with epigenetic regulation and metabolic adaptation. AARS1 catalyzes lysine lactylation via an ATP- and lactate- dependent, but lactyl-CoA-independent mechan...
ORGANISM(S): Homo sapiens (Human) 
2026-07-29 | PXD076410 | Pride
Lactyltransferase Covalent ligand Aars1 
ProteomicsDiscovery and optimisation of a covalent ligand for TRIM25 and its application to targeted protein ubiquitination
The tripartite motif (TRIM) family of RING-type E3 ligases catalyses the formation of many different types of ubiquitin chains, and as such, plays important roles in diverse cellular functions, ranging from immune regulation to cancer signalling pathways. Few ligands have been discovered for TRIM E3...
ORGANISM(S): Homo sapiens (Human) 
2025-05-19 | PXD061182 | Pride
Covalent ligand E3 ligase Ubiquitin Ia-dtb 
ProteomicsABPP-LC/MS results of covalent inhibitor targeting LC3A/B in HeLa cells
The autophagic ubiquitin-like protein LC3 functions through interactions with LC3-interaction regions (LIRs) of other autophagy proteins including autophagy receptors, which stands out as a promising protein-protein interaction (PPI) target for the intervention of autophagy. Through screening covale...
ORGANISM(S): Homo sapiens (Human) 
2023-03-11 | PXD026874 | Pride
Abpp Lc3 Autophagy Covalent 
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 
GenomicsTarget discovery by covalent phenotypic screening in a stem cell differentiation model
Target discovery by covalent phenotypic screening in a stem cell differentiation model
PRJNA1399351 | ENA
GenomicsDevelopment of potent and selective KDM5 covalent inhibitors
Histone lysine demethylase (KDMs) are involved in the dynamic regulation of gene expression by reversible regulation of the methylation levels on lysine residues in histone tails. Among the KDMs, the jumonji (JmjC)-domain-containing KDMs (KDM2-7) are Fe(II), 2- OG (α-ketoglutarate) and molecular oxy...
ORGANISM(S): Homo sapiens 
2018-12-10 | GSE118589 | GEO
ProteomicsSystematic cysteine scanning identifies a druggable pocket in oncogenic KRAS
We developed Cysteine Mapping of Accessible Pockets (CysMAP), a method for identifying druggable pockets in proteins. CysMAP employs systematic pooled cysteine variant libraries screened against diverse covalent compound libraries by intact LC-MS. Here, we applied CysMAP to 189 KRAS(G12D) variants, ...
ORGANISM(S): Homo sapiens (Human) 
2026-02-05 | PXD073201 | Pride
UnknownChemical Aristocracy: He3 Dication and Analogous Noble-Gas-Exclusive Covalent Compounds.
Not available
S-EPMC11017316 | biostudies-literature
TranscriptomicsTarget discovery by covalent phenotypic screening in a stem cell differentiation model
We performed a high throughput screen of a newly curated covalent fragment library comprising 894 compounds. The phenotypic screen was designed to identify signalling pathway modulators and constituted a differentiation assay whereby primed human induced pluripotent cells (iPSCs) were differentiated...
ORGANISM(S): Homo sapiens 
2026-09-28 | GSE315812 | GEO
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