Article
Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase.
Molecular and cellular endocrinology - 5 Sept 2013
Mologni Luca, Redaelli Sara, Morandi Andrea, Plaza-Menacho Ivan, Gambacorti-Passerini Carlo
Abstract excerpt
RET kinase is aberrantly activated in thyroid cancers and in rare cases of lung and colon cancer, and has been validated as a molecular target in these tumors. Vandetanib was recently approved for the treatment of medullary thyroid cancer. However, vandetanib is ineffective in vitro against RET mutants carrying bulky aminoacids at position 804, the gatekeeper residue, similarly to drug-resistant BCR-ABL mutants...
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