GCN2 kinase activation by ATP-competitive kinase inhibitors

Mellinghoff I, Tang CP, Clark O, Ferrarone J, Campos C, Lalani AS, Chodera JD, Intlekofer AM, and Elemento O
Nature Chemical Biology}, 18:207, 2022 [DOI]

We describe paradoxical activation of GCN2 kinase activity by the kinase inhibitor neratinib, and propose a model for how inhibitor-induced dimerization might cause this unusual activity.