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ProteomicsBRD4 degradation via stabilization of a native interaction with DCAF16
Targeted protein degradation is a modality based on small molecules that induce proximity between a protein of interest (POI) and an E3 ubiquitin ligase, thus prompting POI ubiquitination and degradation. To expand the reach of TPD, current research is geared to unlock novel E3s. To that end, the tr...
ORGANISM(S): Homo sapiens (Human) 
2024-01-08 | PXD040570 | Pride
Brd4 degradation Kbm7 Small molecule induced proximity Chemical proteomics Gne-0011 Protac Orbitrap fusion lumos Lc-ms/ms 
ProteomicsMechanistic basis for selective Mediator-dependence of cell type-specifying transcription
The Mediator complex routes signals from DNA-binding transcription factors to RNA polymerase (Pol) II. Despite its pivotal position, mechanistic understanding of Mediator in human cells remains incomplete. Here, we quantified Mediator-controlled Pol II kinetics by coupling rapid subunit degradation ...
ORGANISM(S): Homo sapiens (Human) 
2021-09-08 | PXD017611 | Pride
Chromatin proteomics Human Chromatome Lumos 
ProteomicsTAK285 induced degradation – selectivity profiling in NALM-6 cells
The hit compound TAK285 was subjected to full proteome profiling by TMTpro 6-plex to assess its degradation selectivity in NALM-6 cells. TAK285 induced the degradation of the kinase BLK. The compound was further mechanistically dissected as reported with orthogonal assays such as FACS-based CRISPR/C...
ORGANISM(S): Homo sapiens (Human) 
2025-09-04 | PXD059599 | Pride
Kinase inhibitors Tmt 
ProteomicsProbing kinase proximity interactome modulation upon drug treatment by miniTurboID proximity labelling
In a systematic effort to profile kinase inhibitors, which also act as degraders, we identified multiple hit compounds. These were subjected to detailed mechanism of action elucidation including analysis of the perturbed interactome and its effect on degradation. For our first example, LYN, Src inhi...
ORGANISM(S): Homo sapiens (Human) 
2025-09-04 | PXD062184 | Pride
Kinase inhibitors Tmt 
ProteomicsSelectivity profiling of inhibitor treated human cells via full proteome profiling
Three selective hit compounds from an arrayed kinome abundance screen (98 kinases vs 1570 kinase inhibitors) were subjected to full proteome profiling by TMTpro 18-plex to assess their degradation selectivity in K562 cells. Src inhibitor 3 showed the most significant downregulation of the target kin...
ORGANISM(S): Homo sapiens (Human) 
2025-06-09 | PXD053130 | Pride
K562 Kinase inhibitors Monovalent degrader Tmt 
ProteomicsWithanolide analogues disrupt a leukemic dependency on cholesterol transport by inhibiting the oxysterol-binding protein OSBP (TPP)
Metabolic alterations in cancers precipitate in associated dependencies that can be therapeutically exploited. To meet this goal, natural product inspired small molecules can provide a resource of underexplored chemotypes. We identify W7, a synthetic withanolide analog with pronounced anti-leukemic ...
ORGANISM(S): Homo sapiens (Human) 
2024-06-27 | PXD040692 | Pride
Thermal proteome profiling Expression proteomics Withanolides Natural product-inspired compound libraries 
ProteomicsWithanolide analogues disrupt a leukemic dependency on cholesterol transport by inhibiting the oxysterol-binding protein OSBP (Expression proteomics)
Metabolic alterations in cancers precipitate in associated dependencies that can be therapeutically exploited. To meet this goal, natural product inspired small molecules can provide a resource of underexplored chemotypes. We identify W7, a synthetic withanolide analog with pronounced anti-leukemic ...
ORGANISM(S): Homo sapiens (Human) 
2024-06-27 | PXD040694 | Pride
Thermal proteome profiling Expression proteomics Withanolides Natural product-inspired compound libraries 
ProteomicsDiscovery of molecular glue degraders via isogenic morphological profiling
Molecular glue degraders (MGDs) are small molecules that degrade proteins-of-interest via the ubiquitin-proteasome system. Historically, MGDs were discovered serendipitously. Current approaches for MGD discovery include cell-viability based drug screens or data mining of public transcriptomics and d...
ORGANISM(S): Homo sapiens (Human) 
2023-11-20 | PXD045892 | Pride
Neo-substrate Cereblon Targeted protein degradation Molecular glue degrader E3 ubiquitin ligase 
ProteomicsChemoproteomic selectivity profiling of TAK285 in NALM6 cells
We used dose-dependent chemoproteomic competition assays to profile the proteome-wide target binding and selectivity of the kinase inhibitor TAK285.
ORGANISM(S): Homo sapiens (Human) 
2025-10-06 | PXD064676 | Pride
Lc-ms/ms 
ProteomicsLarge-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells
Chemical modulation of protein function enables a mechanistic understanding of biological circuits and represents the foundation of most medicines. However, despite major efforts over decades of research, around 80% of the human proteome still lack functional ligands. Chemical proteomics allowed the...
ORGANISM(S): Homo sapiens (Human) 
2024-05-07 | PXD041587 | Pride
Machine learning Bioactive Drug Screening Chemical probe Fragment-protein interaction Fbld Ai Chemical proteomics Ligandability 
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