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Molecules 2018, 23(2), 285; doi:10.3390/molecules23020285

PTEN Inhibition in Human Disease Therapy

Biomarkers in Cancer Unit, Biocruces Health Research Institute, 48903 Barakaldo, Spain
IKERBASQUE, Basque Foundation for Science, 48013 Bilbao, Spain
Received: 10 January 2018 / Revised: 26 January 2018 / Accepted: 28 January 2018 / Published: 30 January 2018
(This article belongs to the Special Issue Protein-Tyrosine Phosphatase Inhibitors)
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The tumor suppressor PTEN is a major homeostatic regulator, by virtue of its lipid phosphatase activity against phosphatidylinositol 3,4,5-trisphosphate [PI(3,4,5)P3], which downregulates the PI3K/AKT/mTOR prosurvival signaling, as well as by its protein phosphatase activity towards specific protein targets. PTEN catalytic activity is crucial to control cell growth under physiologic and pathologic situations, and it impacts not only in preventing tumor cell survival and proliferation, but also in restraining several cellular regeneration processes, such as those associated with nerve injury recovery, cardiac ischemia, or wound healing. In these conditions, inhibition of PTEN catalysis is being explored as a potentially beneficial therapeutic intervention. Here, an overview of human diseases and conditions in which PTEN inhibition could be beneficial is presented, together with an update on the current status of specific small molecule inhibitors of PTEN enzymatic activity, their use in experimental models, and their limitations as research or therapeutic drugs. View Full-Text
Keywords: small molecule PTEN inhibitor; neuroregeneration; tissue injury; wound healing; response to infection; infertility; stem-cells; cancer; diabetes; pain relief small molecule PTEN inhibitor; neuroregeneration; tissue injury; wound healing; response to infection; infertility; stem-cells; cancer; diabetes; pain relief

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Pulido, R. PTEN Inhibition in Human Disease Therapy. Molecules 2018, 23, 285.

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