PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting

Nat Rev Cancer. 2015 Jan;15(1):7-24. doi: 10.1038/nrc3860.


Phosphatidylinositol 3-kinases (PI3Ks) are crucial coordinators of intracellular signalling in response to extracellular stimuli. Hyperactivation of PI3K signalling cascades is one of the most common events in human cancers. In this Review, we discuss recent advances in our knowledge of the roles of specific PI3K isoforms in normal and oncogenic signalling, the different ways in which PI3K can be upregulated, and the current state and future potential of targeting this pathway in the clinic.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Drug Resistance, Neoplasm
  • Humans
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / physiology
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy
  • Neoplasms / enzymology*
  • Phosphatidylinositol 3-Kinases / physiology*
  • Phosphatidylinositol Phosphates / metabolism
  • Phosphoinositide-3 Kinase Inhibitors
  • Signal Transduction


  • Antineoplastic Agents
  • Isoenzymes
  • Phosphatidylinositol Phosphates
  • Phosphoinositide-3 Kinase Inhibitors