Isoform-Selective Targeting of Akt Through Covalent Allosteric Inhibition.
Developing selective covalent-allosteric Akt inhibitors targeting Akt2 and Akt3 while sparing Akt1 is reported, which establishes a framework for the development of isoform-selective therapeutics and highlights the potential for unraveling isoform-specific functions in signaling pathways relevant to cancer biology.