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Profiling of the drug resistance of thousands of Src tyrosine kinase mutants uncovers a regulatory network that couples autoinhibition to catalytic domain dynamics

2021-12-06

Abstract excerpt

<h4>SUMMARY</h4> Kinase inhibitors are effective cancer therapies but resistance often limits clinical efficacy. Despite the cataloguing of numerous resistance mutations, our understanding of kinase inhibitor resistance is still incomplete. Here, we comprehensively profiled the resistance of ∼3500 Src tyrosine kinase mutants to four different ATP-competitive inhibitors. We found that ATP-competitive inhibitor res...

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Literature Corpus work
bbf6eceb-ba9b-5954-8f71-6232c4105b16
DOI
10.1101/2021.12.05.471322
Open publication

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Profiling of the drug resistance of thousands of Src tyrosine kinase mutants uncovers a regulatory network that couples autoinhibition to catalytic domain dynamicsDOI 10.1101/2021.12.05.471322
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