Products/Services Used | Details | Operation |
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Gene Synthesis> | For low-throughput validation, full-length WT and mutant CDK6 for K443M, D104S, F98E, F28R, G25S, T58F and V45M were synthesized in pdonor223 without codon optimization and without stop codons (GenScript)... | Get A Quote |
Kinases are involved in disease development and modulation of their activity can be therapeutically beneficial. Drug-resistant mutant kinases are valuable tools in drug discovery efforts, but the prediction of mutants across the kinome is challenging. Here, we generate deep mutational scanning data to identify mutant mammalian kinases that drive resistance to clinically relevant inhibitors. We aggregate these data with subsaturation mutagenesis data and use it to develop, test and validate a framework to prospectively identify residues that mediate kinase activity and drug resistance across the kinome. We validate predicted resistance mutations in CDK4, CDK6, ERK2, EGFR and HER2. Capitalizing on a highly predic... More