Therapeutic potential of phosphoinositide 3-kinase inhibitors

Chem Biol. 2003 Mar;10(3):207-13. doi: 10.1016/s1074-5521(03)00048-6.


At least one Holy Grail for many academic researchers and pharmaceutical research divisions alike has been to identify therapeutically useful selective PI3K inhibitors. There are several different but closely related PI3Ks which are thought to have distinct biological roles. Until now, however, researchers have been frustrated by poor selectivity of the available pharmacological inhibitors, which are unable to distinguish the different isoforms of PI3K adequately. Fortunately, recently published work gives cause for optimism; there are now several patent specifications published that describe new PI3K inhibitors, including some that are more selective for the delta isoform of PI3K. Given the involvement of PI3Ks in a plethora of biological settings, such isoform-selective inhibitors may have immense potential use for the treatment of patients with inflammatory and autoimmune disorders as well as cancer and cardiovascular diseases.

Publication types

  • Review

MeSH terms

  • Autoimmune Diseases / drug therapy
  • Autoimmune Diseases / enzymology
  • Cardiovascular Diseases / drug therapy
  • Cardiovascular Diseases / enzymology
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Inflammation / drug therapy
  • Inflammation / enzymology
  • Isoenzymes / antagonists & inhibitors
  • Neoplasms / drug therapy
  • Neoplasms / enzymology
  • Phosphoinositide-3 Kinase Inhibitors*
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Isoenzymes
  • Phosphoinositide-3 Kinase Inhibitors