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PDK1 inhibitors act on 3-phosphoinositide-dependent protein kinase 1 (PDK1), an upstream growth-signaling kinase. PDK1 was characterized as the kinase that phosphorylates and activates protein kinase B (AKT) once phosphoinositide lipids accumulate at the membrane. It also phosphorylates the activation loop of related kinases in the protein kinase A, G and C (AGC) group, including p70 S6 kinase and protein kinase C isoforms. Listed inhibitors include GSK 2334470 and OSU-03012, while BX-795 and BX-912 also block other kinases. PHT-427 targets both AKT and PDK1, and PS 48 is a PDK1 activator used to study the opposite effect.
