PDK1 inhibitors

Pharm Pat Anal. 2012 May;1(2):145-63. doi: 10.4155/ppa.12.17.


PDK1 is a key member of the AGC protein kinase family. It plays an important role in a variety of cellular functions, leading to the activation of the PI3K signaling pathway, an event often associated with the onset and progression of several human cancers. Numerous recent observations suggest that PDK1 inhibitors may provide novel opportunities for the development of effective classes of therapeutics. On these premises, recent years have witnessed an increased effort by medicinal chemists to develop novel scaffolds to derive potent and selective PDK1 inhibitors. The intent of this review is to update the reader on the recent patent literature, covering applications published between June 2008 and September 2011 that report on PDK1 inhibitors.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • 3-Phosphoinositide-Dependent Protein Kinases / antagonists & inhibitors*
  • Animals
  • Antineoplastic Agents / pharmacology
  • Drug Design*
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / pathology
  • Patents as Topic
  • Phosphatidylinositol 3-Kinases / metabolism
  • Protein Kinase Inhibitors / pharmacology*
  • Signal Transduction / physiology


  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Phosphatidylinositol 3-Kinases
  • 3-Phosphoinositide-Dependent Protein Kinases
  • PDPK1 protein, human