Original paper
Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders
Abstract
The serine/threonine kinase AKT functions as a critical node of the phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of rapamycin (m-TOR) signaling pathway. Aberrant activation and overexpression of AKT are strongly correlated with numerous human cancers. To date, only two AKT degraders with no structure–activity relationship (SAR) results have been reported. Through extensive SAR studies on various linkers, E3 ligase ligands, and AKT...
Paper Details
Title
Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders
Published Date
Dec 2, 2021
Volume
64
Issue
24
Pages
18054 - 18081