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- W2011519297 abstract "PTEN is a tumor suppressor mutated in a large variety of human tumor cells. It antagonizes the PI3K signaling pathway by dephosphorylating the PI(3,4,5)P3 at the 3 position of the inositol ring and plays an important role in cell growth, proliferation, survival and motility. 3-Deoxy-PI derivatives have cytotoxic activity against various human cancer cell lines by a mechanism thought to involve reduced Akt1 phosphorylation. However, these molecules could act as inhibitors of PTEN. A series of D-3-deoxy-PI derivatives and their enantiomers (3-deoxy-diC8PI, 3,5-dideoxy-diC8PI and diC8PI) had been synthesized and studied as inhibitors of PTEN catalyzed hydrolysis of PI(3)P substrates. With diC8PI(3)P as the substrate, the L- enantiomers are usually not as good inhibitors as the D- compounds, although there is an increase in potency with increasing deoxygenation. The short-chain lipids exist in the assay solution as a mix of mostly monomers but with some small micelles. By using D-diC16PI(3)P as the substrates, the effect of the aggregation state of the substrates was also checked. When the substrates are presented to PTEN in micelles with TX-100, none of the 3-deoxy-PI derivatives are good inhibitors. However, when the substrates are presented in large unilamellar vesicles, the inhibitory behavior of the 3-deoxy-PI derivatives is similar to what was observed in the diC8PI(3)P monomer/micelle system. The binding behavior of PTEN to PI vesicles in the presence of the deoxy-PI analogs has also been studied using FRET. The results showed that for the L-series, deoxygenation on the inositol head group increases the potency of enhancing the protein binding to the vesicles. In this case, L-3,5-dideoxy-diC8PI can enhance binding by 50% at the lower concentration, while L-diC8PI can only enhance binding at the high concentration larger than 1mM. These results are used to assess lipid binding sites in PTEN." @default.
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- W2011519297 date "2009-02-01" @default.
- W2011519297 modified "2023-10-05" @default.
- W2011519297 title "PTEN Inhibition Study by Synthetic 3-Deoxy-PI Derivatives" @default.
- W2011519297 doi "https://doi.org/10.1016/j.bpj.2008.12.2262" @default.
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