PTEN

PTEN

PTEN is a heavily studied lipid phosphatase and tumour suppressor. It metabolizes PtdIns(3,4,5)P3,the principal product of the class I PI3-Kinases and thus inhibits the activation of the growth-promoting PI3K-AKT signalling pathway.

An overview of PTEN

PTEN (phosphatase and tensin homolog deleted on chromosome ten),which is located on a chromosome 10q23.3, consisting of nine exons. It can encode proteins composed of 403 amino acids and has the activity of phosphatase. It belongs to the protein tyrosine phosphatases gene family.

The protein products contain a functional area of casein phosphatase and about 175 amino acids, which are homologous with skeleton proteins tenasin and auxilin. The phosphatase functional areas of PTEN include (I/V) -h-c-x-a-g-x-x-r-(S/T) -g molds, which are also found in tyrosine and dual-specifity phosphatases.

Inhibitor of PTEN

I is a potent and specific phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor.

III β-Glycerol phosphate disodium salt pentahydrate is a Phosphatase and tensin homolog (PTEN) inhibitor extracted from patent US 20110002877 A1.

The clinicalsignificance of PTEN

PTEN protein can inhibit tumor development by antagonizing the activity of phosphorylase such as tyrosine kinase. The results showed that the growth and invasion ability of tumor cells was significantly inhibited after transfection of wild-type PTEN gene to glioblastoma with abnormal glioblastoma. Therefore, it is speculated that it can significantly inhibit the activity of focal adhesion kinase (FAK) in tumor cells. In addition, PTEN protein also can indirectly inhibit insulin-induced inositol -3 kinase activity by specifically dephosphorylating IP3's third phosphoric acid. IP3 is an important second messenger in the signaling pathway of insulin regulating cell growth, indicating that PTEN protein plays an important role in the signaling pathway of cell growth. Mutations in the PTEN gene can also cause a range of diseases. Therefore, it has very important clinical significance.

The present studies have found that PTEN gene abnormality can be found in glioblastoma, prostate cancer, endometrial cancer, kidney cancer, ovarian cancer, breast cancer, lung cancer, bladder cancer, thyroid cancer, head and neck squamous cell carcinoma, melanoma, lymphoma etc. In a variety of tumors, PTEN gene is considered as another gene after the P53 gene which involves relatively broad changes and is closely associated with tumor suppressor genes. PTEN gene is deactivated mainly by allele deletion, gene mutation and methylation. PTEN gene is an evaluation index of prognosis of many tumors. It is of great importance to study its mechanism for tumor diagnosis and gene therapy.

References:

1. Luo, H. R., & Li, Y. (2011). U.S. Patent Application No. 12/497,629.

2. Furnari, F. B., Huang, H. S., & Cavenee, W. K. (1998). The phosphoinositol phosphatase activity of PTEN mediates a serum-sensitive G1 growth arrest in glioma cells. Cancer Research, 58 (22), 5002-5008.

3. Cantley, L. C., & Neel, B. G. (1999). New insights into tumor suppression: PTEN suppresses tumor formation by restraining the phosphoinositide 3-kinase/AKT pathway. Proceedings of the National Academy of Sciences, 96 (8), 4240-4245.

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