PTEN公司
PI3K/AKT/mTOR通路
蛋白激酶B
癌症研究
生物
基因沉默
磷酸酶
细胞生物学
信号转导
磷酸化
遗传学
基因
作者
Amancio Carnero,Carmen Blanco‐Aparicio,Oliver Renner,Wolfgang Link,Juan Fernando Martínez-Leal
出处
期刊:Current Cancer Drug Targets
[Bentham Science]
日期:2008-05-01
卷期号:8 (3): 187-198
被引量:762
标识
DOI:10.2174/156800908784293659
摘要
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
科研通智能强力驱动
Strongly Powered by AbleSci AI