Proximity-induced rewiring of oncogenic kinase triggers apoptosis

Abstract excerpt

<h4>ABSTRACT</h4> The active site’s electric field is integral to enzymatic catalysis (e.g., substrate recognition) and nature employs charge-altering post-translational modifications (e.g., phosphorylation) to perturb this electric field and regulate enzymes. A chromosomal translocation converts Abelson kinase (ABL) to BCR-ABL, whose hyperactivity drives several cancers. Here, we developed a small molecule, BRD8...

Topics

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• Chronic Myeloid Leukemia Treatments
• Drug Design
• Mutation
• Neoplasms
• Peptidase Inhibition and Analysis
• Protein Conformation
• Protein Degradation and Inhibitors
• Ubiquitin and proteasome pathways

Identifiers and source

Literature Corpus work

0a829619-519c-5a13-93fa-0487390399e3

DOI

10.1101/2025.06.13.659082