PTEN is a tumor suppressor that inhibits the PI3K/AKT pathway. PTEN inhibitors, such as bisperoxovanadium, can enhance the PI3K/AKT pathway to promote cell migration, survival and proliferation. While there are some concerns over possible cell cycle dysregulation and tumorigenesis, temporary and moderate PTEN inhibition may confer neuroprotection against traumatic brain injury and improve CNS recovery by reestablishing lost connections by axonogenesis. Medicinal value of PTEN inhibitors remains to be determined.