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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
Main proteases and papain-like proteases (PLpro) are essential coronaviral enzymes required for polypeptide processing during viral maturation. PLpro additionally cleave host cellular proteins to evade anti-viral immune responses. Here, we provide biochemical, structural and functional characterizat...
ORGANISM(S): Homo sapiens (Human) 
2020-08-05 | PXD018983 | Pride
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
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
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

The induction of endoplasmic reticulum unfolded protein responses (UPRER) contributes to cancer development and progression. We recently linked microbiota-related triggers to the tumor-promoting role of signal transducer activating transcription factor 6 (ATF6) in the colon. Here we substantiate ...

2025-07-02 | MTBLS7387 | MetaboLights
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