Article
Mutant-selective AKT inhibition through lysine targeting and neo-zinc chelation.
Nature - 1 Jan 2025
Craven Gregory B, Chu Hang, Sun Jessica D, Carelli Jordan D, Coyne Brittany, Chen Hao, Chen Ying, Ma Xiaolei, Das Subhamoy, Kong Wayne, Zajdlik Adam D, Yang Kin S, Reisberg Solomon H, Thompson Peter A, Lipford J Russell, Taunton Jack
Abstract excerpt
Somatic alterations in the oncogenic kinase AKT1 have been identified in a broad spectrum of solid tumours. The most common AKT1 alteration replaces Glu17 with Lys (E17K) in the regulatory pleckstrin homology domain1, resulting in constitutive membrane localization and activation of oncogenic signalling. In clinical studies, pan-AKT inhibitors have been found to cause dose-limiting hyperglycaemia2-6, which has...
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