Defining the landscape of ATP-competitive inhibitor resistance residues in protein kinases
Persky NS, Hernandez D, Do Carmo M, Brenan L, Cohen O, Kitajima S, Nayar U, Walker A, Pantel S, Lee Y, Cordova J, Sathappa M, Zhu C, Hayes TK, Ram P, Pancholi P, Mikkelsen TS, Barbie DA, Yang X, Haq R, Piccioni F, Root DE, Johannessen CM. Defining the landscape of ATP-competitive inhibitor resistance residues in protein kinases. Nature Structural & Molecular Biology 2020, 27: 92-104. PMID: 31925410, DOI: 10.1038/s41594-019-0358-z.Peer-Reviewed Original ResearchConceptsMammalian kinasesDeep mutational scanning dataDrug discovery effortsProtein kinaseMutagenesis dataMutant kinasesKinase activityDrug resistanceKinomeKinaseDiscovery effortsRelevant inhibitorsResiduesDisease developmentResistance mutationsMutationsActivation siteERK2MEK1MutantsBroader interrogationInhibitorsCSNK2A1Valuable toolTBK1