Article
A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity.
British journal of cancer - 1 Aug 2020
Kostaras Eleftherios, Kaserer Teresa, Lazaro Glorianne, Heuss Sara Farrah, Hussain Aasia, Casado Pedro, Hayes Angela, Yandim Cihangir, Palaskas Nicolaos, Yu Yi, Schwartz Brian, Raynaud Florence, Chung Yuen-Li, Cutillas Pedro R, Vivanco Igor
Abstract excerpt
BACKGROUND: AKT, a critical effector of the phosphoinositide 3-kinase (PI3K) signalling cascade, is an intensely pursued therapeutic target in oncology. Two distinct classes of AKT inhibitors have been in clinical development, ATP-competitive and allosteric. Class-specific differences in drug activity are likely the result of differential structural and conformational requirements governing efficient target...
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