Resistance to kinase inhibition through shortened target engagement

Imatinib, a selective inhibitor of the breakpoint cluster region (BCR)-ABL kinase, is the poster child for targeted cancer therapeutics. However, its efficacy is limited by resistance mutations. Using a quantitative bioluminescence resonance energy transfer assay in living cells, we identified ABL k...

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Detalles Bibliográficos
Autores principales: Rangwala, Aziz M., Berger, Benedict-Tilman, Robers, Matthew B., Knapp, Stefan, Seeliger, Markus A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2022
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Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8890393/
https://www.ncbi.nlm.nih.gov/pubmed/35252553
http://dx.doi.org/10.1080/23723556.2022.2029999
Descripción
Sumario:Imatinib, a selective inhibitor of the breakpoint cluster region (BCR)-ABL kinase, is the poster child for targeted cancer therapeutics. However, its efficacy is limited by resistance mutations. Using a quantitative bioluminescence resonance energy transfer assay in living cells, we identified ABL kinase mutations that could cause imatinib resistance by altering drug residence time.

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