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ProteomicsThermal proteome profilng of BMAL1 ligand CCM in U2OS cell lysate
The master transcription factor BMAL1-CLOCK is crucial for orchestrating rhythmic gene expression and governing circadian rhythms. Pharmacological manipulation of this central circadian regulator requires accessible protein cavities and selective compounds. By targeting BMAL1 through a resident cav...
ORGANISM(S): Homo sapiens (Human) 
2025-02-03 | PXD049298 | Pride
Thermal proteome profiling 
ProteomicsAffinity-based chemoproteomic profiling of UNC0638 and UNC0737 in MCF7 and PBMC lysates identifies CHKA as a shared off-target.
To identify the molecular target(s) and elucidate the mechanism of action of UNC0638 and UNC0737, affinity-based chemoproteomics was performed. UNC0965, a biotinylated analogue of UNC0638, was immobilised on streptavidin-coated sepharose beads to enrich binding proteins from whole MCF7 or PBMC cell ...
ORGANISM(S): Homo sapiens (Human) 
2025-01-27 | PXD056865 | Pride
Chemical proteomics 
ProteomicsPlant homeodomain targeting cyclic peptides allosterically modulate KDM7 histone demethylase activity
Here we report the discovery of a set of potent de-novo cyclic peptides (CPs) targeting different binding sites on KDM7B. One CP (OC9) bound directly to the KDM7 PHD-finger, as supported by bio-layer interferometry (BLI), isothermal calorimetry (ITC), hydrogen-deuterium exchange mass spectrometry (H...
ORGANISM(S): Homo sapiens (Human) 
2023-07-20 | PXD027151 | Pride
Kdm7 Proteomics Cyclic peptide Ptm 
ProteomicsA Chemical Biology Toolbox to Study Protein Methyltransferases and Epigenetic Signaling
Protein methyltransferases (PMTs) comprise a major class of epigenetic regulatory enzymes with therapeutic relevance. Here we present a collection of chemical probes and associated reagents and data to elucidate the function of human and murine PMTs in cellular studies. Our collection provides inhib...
ORGANISM(S): Homo sapiens (Human) 
2018-12-19 | PXD009028 | Pride
Lfq Epigenetics Chemical probes 
ProteomicsA BRET Biosensor for Measuring Uncompetitive Engagement of PRMT5 Complexes in Cells
Protein arginine methyl transferase 5 (PRMT5) plays a global role in cell physiology and is an established therapeutic target in cancer. In approximately 10-15% of human cancers, deletion of the methylthioadenosine phosphorylase (MTAP) gene results in accumulation of methylthioadenosine (MTA), expos...
ORGANISM(S): Homo sapiens (Human) 
2025-12-08 | PXD028138 | Pride
Nanobret - chemical proteomics – cell-based assay – sam – target engagement – thermal profiling 
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