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Current Cancer Drug Targets


ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

The PTEN/PI3K/AKT Signalling Pathway in Cancer, Therapeutic Implications

Author(s): Amancio Carnero, Carmen Blanco-Aparicio, Oliver Renner, Wolfgang Link and Juan F.M. Leal

Volume 8, Issue 3, 2008

Page: [187 - 198] Pages: 12

DOI: 10.2174/156800908784293659

Price: $65


PTEN/PI3K/AKT constitutes an important pathway regulating the signaling of multiple biological processes such as apoptosis, metabolism, cell proliferation and cell growth. PTEN is a dual protein/lipid phosphatase which main substrate is the phosphatidyl-inositol,3,4,5 triphosphate (PIP3), the product of PI3K. Increase in PIP3 recruits AKT to the membrane where it is activated by other kinases also dependent on PIP3. Many components of this pathway have been described as causal forces in cancer. PTEN activity is lost by mutations, deletions or promoter methylation silencing at high frequency in many primary and metastatic human cancers. Germ line mutations of PTEN are found in several familial cancer predisposition syndromes. Activating mutations which have been reported for PI3K and AKT, in tumours are able to confer tumourigenic properties in several cellular systems. Additionally, the binding of PI3K to oncogenic ras is essential for the transforming properties of ras. In summary, the data strongly support the view of the PTEN/PI3K/AKT pathway as an important target for drug discovery.

Keywords: PTEN, PI3K, AKT, cancer therapeutics, drug discovery

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