• Antagonized the oncogenic PI3K/AKT/S6K pathway in vivo • Inhibited growth of lung cancer cells • Decreased off-target effects • Effectively regulated PTEN activity • Applicable to diseases driven by compromised PTEN functions
USF researchers have synthesized a novel class of peptidomimetic (.gamma.-AApeptides) compounds that can regulate PTEN activity. Results have shown that these peptides enhance PTEN lipid phosphatase activity in vitro and antagonize the PI3K/AKT/S6K pathway in vivo. Furthermore, treatment with the small molecules reduced cell proliferation and migration and induced cell cycle arrest in lung cancer cells. These novel compounds present an improved therapeutic approach to circumvent off-target effects and drug resistance associated with current kinase inhibition modalities, applicable to diseases driven by compromised PTEN functions.
Dose-Dependent Effects on Proliferation and Cell Cycle Arrest Using Two Novel Peptidomimetics in Lung Adenocarcinoma Cells