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Inhibiting PI3K as a therapeutic strategy against cancer

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  • Molecular Targets in Oncology
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Abstract

Class I PI3K is composed of heterodimeric lipid kinases regulating essential cellular functions including proliferation, apoptosis and metabolism. Class I PI3K isoforms are commonly amplified in different cancer types and the PI3Kα catalytic subunit, PIK3CA, has been found mutated in a variable proportion of tumours of different origin. Furthermore, PI3K has been shown to mediate oncogenic signalling induced by several oncogenes such as HER2 or Ras. These facts suggest that PI3K might be a good target for anticancer drug discovery. Today, the rise of PI3K inhibitors and their first in vivo results have cleared much of the path for the development of PI3K inhibitors for anticancer therapy. Here we will review the PI3K pathway and the pharmacological results of PI3K inhibition.

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Authors and Affiliations

  1. Medical Oncology, Hospital Universitario Virgen del Rocío, Sevilla, Spain

    Luis Paz-Ares & Rocío García-Carbonero

  2. Experimental Therapeutics Programme, Spanish National Cancer Research Centre, Madrid, Spain

    Carmen Blanco-Aparicio

  3. Instituto de Biomedicina de Sevilla, Consejo Superior de Investigaciones Científicas, Avda. Manuel Siurot, s/n, ES-41013, Sevilla, Spain

    Amancio Carnero

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  1. Luis Paz-Ares
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  2. Carmen Blanco-Aparicio
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  3. Rocío García-Carbonero
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  4. Amancio Carnero
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Correspondence to Amancio Carnero.

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Supported by an unrestricted educational grant from Pfizer

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Paz-Ares, L., Blanco-Aparicio, C., García-Carbonero, R. et al. Inhibiting PI3K as a therapeutic strategy against cancer. Clin Transl Oncol 11, 572–579 (2009). https://doi.org/10.1007/s12094-009-0407-x

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