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Kinase Inhibitors

2 GoKawiil briefs on this topic

Study describes drug approach that degrades cancer kinases instead of just blocking them

Researchers led by Conery et al., writing in Nature, report a strategy for treating lung cancers driven by mutated kinase enzymes that destroys the target protein entirely rather than merely inhibiting its activity. The approach is aimed at cancers that develop resistance to existing kinase inhibitors after acquiring mutations near the drug's binding site. Twenty-eight kinase inhibitors are already FDA-approved across nine molecular lung cancer subtypes, but many patients eventually relapse due to such resistance mutations.

Researchers detail methods behind bitopic BCR::ABL1 kinase inhibitor study

A methods disclosure describes how researchers sourced and synthesized kinase inhibitors—including ponatinib, asciminib, imatinib, dasatinib and osimertinib—and cultured K562 and HEK293T cell lines to test them. The report details engineered K562 stable lines carrying BCR::ABL1 mutations, created via enzymatic mutagenesis of a pUltra vector, used to evaluate inhibitor activity in cell-based assays.