Development of PROTACs for targeted degradation of oncogenic TRK fusions

Abstract excerpt

Chromosomal translocations leading to the fusion of tropomyosin receptor kinases (TRK) with diverse partner proteins have been identified as oncogenic drivers in many adult and pediatric cancers. While first-generation TRK kinase inhibitors, such as entrectinib and larotrectinib, have shown positive responses in TRK fusion-positive cancers, resistance mutations against these inhibitors in the kinase domain limit t...

Topics

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• Cell Transformation, Neoplastic
• Clinical Trials as Topic
• Drug Resistance, Neoplasm
• Genetic Techniques
• Lung Cancer Treatments and Mutations
• Molecular Targeted Therapy
• Oncogene Proteins, Fusion
• Protein Kinase Inhibitors

Identifiers and source

Literature Corpus work

141bace3-ca52-56ac-8736-0d0f31a25456

DOI

10.1101/2025.06.18.660465