A specific inhibitor of PTEN
Potent inhibitor of PTEN (phosphatase and tensin homolog) (IC50 = 35 nM). Displays selectivity for PTEN over cysteine-based phosphatases such as SopB, MTM, PTPβ and SAC (IC50 values are 588 nM, 4.03, 57.5 and >10 μM respectively). Increases PIP2 and PIP3 levels; also increases Akt translocation in NIH/3T3 fibroblasts. Blocks the immunosuppressant activity of IDO-activated Tregs. Promotes antitumor inflammatory response in combination with immunotherapy and enhances anticancer chemotherapy in tumor-bearing mice.
Rosivatz et al (2006) A small-molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN). ACS Chem.Biol. 1 780 PMID:17240976 |Sharma et al (2015) The PTEN pathway in Tregs is a critical driver of the suppressive tumor microenvironment. Sci.Adv. 1 e1500845 PMID:26601142
动态评分
0.0