The resistance tetrad: amino acid hotspots for kinome-wide exploitation of drug-resistant protein kinase alleles.

Abstract excerpt

Acquired resistance to targeted kinase inhibitors is a well-documented clinical problem that is potentially fatal for patients to whom a suitable back-up is not available. However, protein kinase alleles that promote resistance to inhibitors can be exploited experimentally as gold-standards for "on"- and "off"-target validation strategies and constitute a powerful resource for assessing the ability of new or...

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