PTEN activity is lost by mutations, deletions or promoter methylation silencing at high frequency in many primary and metastatic human cancers. Many components of this pathway have been described as causal forces in cancer. Increase in PIP3 recruits AKT to the membrane where it is activated by other kinases also dependent on PIP3. PTEN is a dual protein/lipid phosphatase which main substrate is the phosphatidyl-inositol,3,4,5 triphosphate (PIP3), the product of PI3K. Experimental Therapeutics Programme, Spanish National Cancer Centre (CNIO), C/Melchor Fernandez Almagro 3, 28029 Madrid, Spain.,SpainĪbstract: PTEN/PI3K/AKT constitutes an important pathway regulating the signaling of multiple biological processes such as apoptosis, metabolism, cell proliferation and cell growth.Title: The PTEN/PI3K/AKT Signalling Pathway in Cancer, Therapeutic ImplicationsĪuthor(s): Amancio Carnero, Carmen Blanco-Aparicio, Oliver Renner, Wolfgang Link and Juan F.M. Keywords: PTEN, PI3K, AKT, cancer therapeutics, drug discovery In summary, the data strongly support the view of the PTEN/PI3K/AKT pathway as an important target for drug discovery. Additionally, the binding of PI3K to oncogenic ras is essential for the transforming properties of ras. Activating mutations which have been reported for PI3K and AKT, in tumours are able to confer tumourigenic properties in several cellular systems. Germ line mutations of PTEN are found in several familial cancer predisposition syndromes. PTEN/PI3K/AKT constitutes an important pathway regulating the signaling of multiple biological processes such as apoptosis, metabolism, cell proliferation and cell growth.
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