Cited by 1,767PI3K/AKT/mTOR signaling in cancerMetabolism, Diabetes, and CancerProtein Kinase Regulation and GTPase Signaling

The emerging mechanisms of isoform-specific PI3K signalling

Vanhaesebroeck, Bart, Guillermet-Guibert, Julie, Graupera, Mariona, Bilanges, Benoit·2010·Nature Reviews Molecular Cell Biology

Abstract

Phosphoinositide 3-kinases (PI3Ks) function early in intracellular signal transduction pathways and affect many biological functions. A further level of complexity derives from the existence of eight PI3K isoforms, which are divided into class I, class II and class III PI3Ks. PI3K signalling has been implicated in metabolic control, immunity, angiogenesis and cardiovascular homeostasis, and is one of the most frequently deregulated pathways in cancer. PI3K inhibitors have recently entered clinical trials in oncology. A better understanding of how the different PI3K isoforms are regulated and control signalling could uncover their roles in pathology and reveal in which disease contexts their blockade could be most beneficial.

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Crossref · 10.1038/nrm2882

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  • The three classes of PI3Ks (I, II and III) differ in substrate specificity, and Class I PI3Ks selectively recognise and phosphorylate PI(4,5)P2.

    “The three classes (Classes I, II and III) of these enzymes differ in their substrate specificity; the Class I PI3Ks selectively recognises and phosphorylates PI(4,5)P2 (reviewed in [60–63]).”

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Authors
Vanhaesebroeck, B., Guillermet-Guibert, J., Graupera, M., & Bilanges, B.
Affiliations
Queen Mary University of London (GB)
Corresponding author
Vanhaesebroeck, Bart
Venue
Nature Reviews Molecular Cell Biology
Published
2010-04-09
Volume
11
Issue
5
Pages
329-341
ISSN
  • 1471-0072 (ISSN-L)
  • 1471-0080
OpenAlex
W2057370954
Cited by
1,767
References
6
Citations by year
2026: 60 · 2025: 106 · 2024: 99 · 2023: 114 · 2022: 106 · 2021: 134 · 2020: 139 · 2019: 124 · 2018: 117 · 2017: 107 · 2016: 105 · 2015: 116 · 2014: 127 · 2013: 98 · 2012: 116
FWCI
8.73
Type
journal article
Language
en
Open access
closed
Locations
  • Nature Reviews Molecular Cell Biology (publishedVersion)
  • PubMed (publishedVersion)
  • UCL Discovery (University College London) (submittedVersion)
Funders
Cancer Research UK
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › PI3K/AKT/mTOR signaling in cancer
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Keywords
phosphatidylinositol 3-kinase, PI3K isoforms, class I PI3K, class II PI3K, class III PI3K, signal transduction, cancer, PI3K inhibitors, metabolic control, immunity, angiogenesis, cardiovascular homeostasis
MeSH terms
Animals, Humans, Isoenzymes, Mutation, Neoplasms, Signal Transduction, Phosphatidylinositol 3-Kinases

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