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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 addition to KIT and PDGFRA mutations, sequential accumulation of other genetic events is involved in the development and progression of gastrointestinal stromal tumors (GISTs). Until recently, the significance of these other alterations has not been thoroughly investigated. The combination of gen...
ORGANISM(S): Homo sapiens 
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
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