The PI3K inhibitor arsenal: choose your weapon!

Trends Biochem Sci. 2007 Oct;32(10):450-6. doi: 10.1016/j.tibs.2007.09.001.


Owing to its widespread activation in inflammation and cancer, a growing appreciation of the therapeutic potential of inhibitors of the phosphoinositide 3-kinase (PI3K) pathway has stimulated intense interest in compounds with suitable pharmacological profiles. These are primarily directed toward PI3K itself. However, as class I PI3Ks are also essential for a range of normal physiological processes, broad spectrum PI3K inhibition could be poorly tolerated. In recent years, patents describing a new generation of PI3K inhibitors have started to appear, with a particular focus on the development of compounds with enhanced isoform selectivity for use as anti-cancer and anti-inflammatory therapies. However, challenges remain for the efforts to pharmacologically target this enzyme family in a successful manner.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Enzyme Activation
  • Inflammation / drug therapy*
  • Inflammation / enzymology
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Phosphoinositide-3 Kinase Inhibitors*
  • Protein Kinase Inhibitors / therapeutic use*


  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Kinase Inhibitors

Associated data

  • RefSeq/NM_008839
  • RefSeq/NM_008840
  • RefSeq/NM_020272
  • RefSeq/NM_029094