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Phosphoinositide-dependent protein kinase 1 (PDK1), also known as PDPK1, is a serine/threonine kinase that plays a central role in cell signaling, growth, and survival. It acts as a "master" upstream kinase that phosphorylates and activates several members of the AGC family of protein kinases, including Akt/PKB, S6 Kinase(s), and RSK. PDK1 functions downstream of PI3-Kinase signaling and its activity is crucial for regulating cell size and development. Small-molecule inhibitors have been developed targeting either the ATP-binding pocket or allosteric sites.
Competitive inhibition at ATP-site or allosteric modulation
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