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OBESITY RESEARCH SOLUTIONSVO-OHpic is a specific inhibitor of phosphatase and tensin homolog (PTEN; IC50 = 35 nM in vitro).1,2 Through this action, it increases cellular phosphatidylinositol 3,4,5-trisphosphate (PIP3) levels, phosphorylation of Akt, and glucose uptake in adipocytes.1 In mice, VO-OHpic (10 µg/kg, i.p.) decreases left ventricular systolic pressure and heart rate and protects against ischemia/reperfusion-induced myocardial infarction.3 VO-OHpic also blocks the development of suppressor activity in regulatory T cells activated with indoleamine 2,3-dioxygenase.4
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1. A small-
2. Characterisation of the PTEN inhibitor VO-
3. PTEN inhibitors cause a negative inotropic and chronotropic effect in mice. Eur. J. Pharmacol. 650(1), 298-302 (2011).
4. The PTEN pathway in Tregs is a critical driver of the suppressive tumor microenvironment. Sci. Adv. 1(10), e1500845 (2015).