Skip to main content

Phosphoinositide 3-Kinase

  • Reference work entry
Encyclopedia of Signaling Molecules
  • 132 Accesses

Synonyms

Phosphatidylinositol 3-kinase; Phosphatidylinositol 3-OH kinase; PI 3-K; PI 3-kinase; PI3K; PI(3)K

Historical Background

Phosphoinositide 3-kinase, commonly abbreviated PI3K, is one of the most well-studied enzymes in the field of signal transduction (Fruman et al. 1998; Vanhaesebroeck et al. 2010). PI3K actually refers to a family of enzymes encoded by eight genes in mammals. Orthologs of one or more PI3K genes exist in all animals as well as in yeast. These enzymes share the ability to phosphorylate the 3′-hydroxyl of the inositol head group of phosphatidylinositol (PtdIns), generating the lipid PtdIns-3-P (Fig. 1). Some members of the PI3K family can act on phosphoinositides, which are phosphorylated derivatives of PtdIns (such as PtdIns-4,5-P2). Therefore, the family is properly referred to as phosphoinositide 3-kinases rather than simply phosphatidylinositol 3-kinases. The products of PI3Ks, generally termed 3-phosphorylated inositides (3-PIs), serve as membrane...

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Institutional subscriptions

References

  • Cantley LC, Auger KR, Carpenter C, Duckworth B, Graziani A, Kapeller R, et al. Oncogenes and signal transduction. Cell. 1991;64:281–302.

    PubMed  CAS  Google Scholar 

  • Deane JA, Fruman DA. Phosphoinositide 3-kinase: diverse roles in immune cell activation. Annu Rev Immunol. 2004;22:563–98.

    PubMed  CAS  Google Scholar 

  • Denley A, Kang S, Karst U, Vogt PK. Oncogenic signaling of class I PI3K isoforms. Oncogene. 2008;27:2561–74.

    PubMed  CAS  Google Scholar 

  • Engelman JA. Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat Rev Cancer. 2009;9:550–62.

    PubMed  CAS  Google Scholar 

  • Engelman JA, Luo J, Cantley LC. The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev Genet.. 2006;7:606–19.

    PubMed  CAS  Google Scholar 

  • Foster KG, Fingar DC. Mammalian target of rapamycin (mTOR): conducting the cellular signaling symphony. J Biol Chem. 2010;285:14071–7.

    PubMed  CAS  Google Scholar 

  • Fruman DA, Bismuth G. Fine tuning the immune response with PI3K. Immunol Rev. 2009;228:253–72.

    PubMed  CAS  Google Scholar 

  • Fruman DA, Meyers RE, Cantley LC. Phosphoinositide kinases. Annu Rev Biochem. 1998;67:481–507.

    PubMed  CAS  Google Scholar 

  • Lemmon MA. Membrane recognition by phospholipid-binding domains. Nat Rev Mol Cell Biol. 2008;9:99–111.

    PubMed  CAS  Google Scholar 

  • Liu P, Cheng H, Roberts TM, Zhao JJ. Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009;8:627–44.

    PubMed  CAS  Google Scholar 

  • Manning BD, Cantley LC. AKT/PKB signaling: navigating downstream. Cell. 2007;129:1261–74.

    PubMed  CAS  Google Scholar 

  • Marone R, Cmiljanovic V, Giese B, Wymann MP. Targeting phosphoinositide 3-kinase: moving towards therapy. Biochim Biophys Acta. 2008;1784:159–85.

    PubMed  CAS  Google Scholar 

  • Salmena L, Carracedo A, Pandolfi PP. Tenets of PTEN tumor suppression. Cell. 2008;133:403–14.

    PubMed  CAS  Google Scholar 

  • Samuels Y, Ericson K. Oncogenic PI3K and its role in cancer. Curr Opin Oncol. 2006;18:77–82.

    PubMed  CAS  Google Scholar 

  • Sparks CA, Guertin DA. Targeting mTOR: prospects for mTOR complex 2 inhibitors in cancer therapy. Oncogene. 2010;29(26):3733–44. Epub April 4.

    PubMed  CAS  Google Scholar 

  • Vanhaesebroeck B, Guillermet-Guibert J, Graupera M, Bilanges B. The emerging mechanisms of isoform-specific PI3K signalling. Nat Rev Mol Cell Biol. 2010;11:329–41.

    PubMed  CAS  Google Scholar 

  • Williams R, Berndt A, Miller S, Hon WC, Zhang X. Form and flexibility in phosphoinositide 3-kinases. Biochem Soc Trans. 2009;37:615–26.

    PubMed  CAS  Google Scholar 

  • Workman P, Clarke PA, Raynaud FI, van Montfort RL. Drugging the PI3 kinome: from chemical tools to drugs in the clinic. Cancer Res. 2010;70:2146–57.

    PubMed  CAS  Google Scholar 

  • Yap TA, Garrett MD, Walton MI, Raynaud F, de Bono JS, Workman P. Targeting the PI3K-AKT-mTOR pathway: progress, pitfalls, and promises. Curr Opin Pharmacol. 2008;8:393–412.

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to David A. Fruman .

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2012 Springer Science+Business Media, LLC

About this entry

Cite this entry

So, L., Fruman, D.A. (2012). Phosphoinositide 3-Kinase. In: Choi, S. (eds) Encyclopedia of Signaling Molecules. Springer, New York, NY. https://doi.org/10.1007/978-1-4419-0461-4_93

Download citation

Publish with us

Policies and ethics