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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 
ProteomicsShotgun proteomics experiments to identify covalent modification of proteins in HCT116 cells by a novel covalent ligand, CL16
By coupling activity-based protein profiling (ABPP) with covalent ligand screening experiment, we have identified a cysteine-reactive covalent ligand, CL16, which can bind strongly and selectively with RhoA in vitro. In this experiment, we performed shotgun proteomics to investigate protein targets ...
ORGANISM(S): Homo sapiens (Human) 
2025-08-30 | PXD053036 | Pride
Protein target identification of a cysteine-reactive covalent ligand In colorectal cancer hct116 cells Cl16 
TranscriptomicsDNA unmethylome profiling by covalent capture of CpG sites
Here we present an approach for the mapping of unmethylated DNA. Our technique is based on DNA methyltransferase-directed transfer of activated groups (mTAG) and covalent biotin tagging of unmodified CpG sites followed by affinity enrichment and interogation on tiling microarrays or next generation ...
ORGANISM(S): Homo sapiens 
2013-08-27 | E-GEOD-48994 | biostudies-arrayexpress
ProteomicsSulfamate acetamides as self-immolative electrophiles for covalent ligand- directed release chemistry
Electrophiles for covalent inhibitors that are suitable for in vivo administration are rare. While acrylamides are prevalent in FDA approved covalent drugs, chloroacetamides are considered too reactive for such purposes. We report sulfamate-based electrophiles that maintain chloroacetamide-like geom...
ORGANISM(S): Homo sapiens (Human) 
2023-03-11 | PXD038301 | Pride
Human Chemical probes Isodtb 
ProteomicsSulfamate acetamides as self-immolative electrophiles for covalent ligand- directed release chemistry - Pull Down data
Electrophiles for covalent inhibitors that are suitable for in vivo administration are rare. While acrylamides are prevalent in FDA approved covalent drugs, chloroacetamides are considered too reactive for such purposes. We report sulfamate-based electrophiles that maintain chloroacetamide-like geom...
ORGANISM(S): Homo sapiens (Human) 
2023-03-11 | PXD038375 | Pride
Human Pull down Chemical probes 
GenomicsEngineering covalent small molecule–RNA complexes in living cells
Engineering covalent small molecule–RNA complexes in living cells
PRJNA1133002 | ENA
TranscriptomicsLigand-Dependent Enhancer Activation Regulated by Topoisomerase-I Activity
The discovery that enhancers are regulated transcription units, encoding eRNAs, has raised new questions about the mechanisms of their activation. Here, we report an unexpected molecular mechanism that underlies ligand-dependent enhancer activation, based on DNA nicking to relieve torsional stress f...
ORGANISM(S): Homo sapiens 
2015-01-22 | E-GEOD-63202 | biostudies-arrayexpress
ProteomicsA group competition strategy for covalent ligand discovery
As a powerful chemoproteomic tool, activity-based protein profiling (ABPP) has been extensively used for covalent ligand discovery. However, the current ABPP-based approaches are inherently based on indirect probe labeling competed by covalent ligands, and cannot directly compare the preferences of ...
ORGANISM(S): Homo Sapiens 
2025-11-06 | PXD070395 |
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 
TranscriptomicsEngineering covalent small molecule–RNA complexes in living cells
Targeting cellular RNA by small molecules has come to the forefront of biotechnology and holds great promise for therapeutic use. Strategies to identify, validate and optimize these molecules are essential, but are still lacking in some aspects. In particular, the site-specific covalent labeling and...
ORGANISM(S): Homo sapiens 
2024-09-30 | GSE271728 | GEO
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