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Article

Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors

8 Sept 2015

Abstract excerpt

Oncogenic ROS1 fusion proteins are molecular drivers in multiple malignancies, including a subset of non-small cell lung cancer (NSCLC). The phylogenetic proximity of the ROS1 and anaplastic lymphoma kinase (ALK) catalytic domains led to the clinical repurposing of the Food and Drug Administration (FDA)-approved ALK inhibitor crizotinib as a ROS1 inhibitor. Despite the antitumor activity of crizotinib observed in...

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PMID: 26372962
DOI: 10.1073/pnas.1515281112

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