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Molecules in medicine mini-review: isoforms of PI3K in biology and disease

  • Molecules in Medicine
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Abstract

The PI3K lipid kinases are involved in signal transduction and intracellular vesicular traffic, endowing these enzymes with multiple cellular functions and important roles in normal physiology and disease. In this mini-review, we aim to distill from the vast PI3K literature the key relevant concepts for successful targeting of this pathway in disease. Of the eight isoforms of PI3K, the class I PI3Ks have been implicated in the aetiology and maintenance of various diseases, most prominently cancer, overgrowth syndromes, inflammation and autoimmunity, with emerging potential roles in metabolic and cardiovascular disorders. The development of class I PI3K inhibitors, mainly for use in cancer and inflammation, is a very active area of drug development. In 2014, an inhibitor of the p110δ isoform of PI3K was approved for the treatment of specific human B cell malignancies. The key therapeutic indications of targeting each class I PI3K isoform are summarized and discussed.

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Acknowledgments

Work in the laboratory of B.V. was supported by Cancer Research UK [C23338/A15965], the UK Biotechnology and Biological Sciences Research Council [BB/I007806/1], the Ludwig Institute for Cancer Research and the National Institute for Health Research (NIHR) University College London Hospitals Biomedical Research Centre.

The authors apologize to those authors whose work could not be cited due to space constraints.

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  1. UCL Cancer Institute, University College London, 72 Huntley Street, London, WC1E 6BT, UK

    Bart Vanhaesebroeck, Maria A. Whitehead & Roberto Piñeiro

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  1. Bart Vanhaesebroeck
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Correspondence to Bart Vanhaesebroeck.

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BV is a consultant to Karus Therapeutics (Oxford, UK).

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Vanhaesebroeck, B., Whitehead, M.A. & Piñeiro, R. Molecules in medicine mini-review: isoforms of PI3K in biology and disease. J Mol Med 94, 5–11 (2016). https://doi.org/10.1007/s00109-015-1352-5

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