PDPK1 is a master kinase, which is crucial for the activation of AKT/PKB and many other AGC kinases including PKC, S6K, SGK. An important role for PDPK1 is in the signalling pathways activated by several growth factors and hormones including insulin signalling. Mice lacking PDPK1 die during early embryonic development, indicating that this enzyme is critical for transmitting the growth-promoting signals nescessary for normal mammalian development.

Mice that are deficient in PDPK1 have a asymp 40% decrease in body mass, mild glucose intolerance, and are resitant to cancer brought about by hyperactivation of the PI3K pathway (PTEN +/-).The structure of PDPK1 can be divided into two domains; the kinase or catalytic domain and the PH domain.