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Efficacy of combination treatment of the inhibitor of phosphatidyl inositol-3-kinase/protein kinase B pathway BEZ235 and the inhibitor of extracellular regulated protein kinase/mitogen-activated protein kinase pathway U0126 in a tumor cell model / 中国医学科学院学报
Acta Academiae Medicinae Sinicae ; (6): 530-534, 2013.
Article in Chinese | WPRIM | ID: wpr-285965
ABSTRACT
<p><b>OBJECTIVE</b>To study the inhibitory effect of the dual usage of BEZ235 and U0126, the inhibitor of phosphatidyl inositol-3-kinase/protein kinase B pathway and extracellular regulated proteinkinase/mitogen-activated protein kinase pathway, respectively, on cell proliferation.</p><p><b>METHODS</b>Phosphatase and tensin homolog knockout mouse embryonic fibroblast (PTEN-/-MEF) cell lines were used as the cellular model for malignant tumors. BEZ235, the dual inhibitor of phosphatidyl inositol-3-kinase and mammalian target of rapamycin, and U0126, the inhibitor of mitogen-activated protein kinase were used to treat the cells individually and in a combination manner. The inhibitory effects to cell proliferation were monitored by MTT.</p><p><b>RESULTS</b>Both BEZ235 and U0126 suppressed PTEN knockout cell proliferation, and their half inhibitory concentrations were 6.257 nmol/L and 22.85 μmol/L, respectively. However, the combination treatment of the two drugs showed antagonistic rather than synergistic effect on cell proliferation.</p><p><b>CONCLUSION</b>BEZ235 and U0126 are not suitable for a combined target therapy regimen.</p>
Subject(s)
Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Quinolines / Butadienes / Cell Line / Mice, Knockout / Cell Proliferation / Drug Antagonism / Phosphatidylinositol 3-Kinase / Fibroblasts / Imidazoles Limits: Animals Language: Chinese Journal: Acta Academiae Medicinae Sinicae Year: 2013 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Quinolines / Butadienes / Cell Line / Mice, Knockout / Cell Proliferation / Drug Antagonism / Phosphatidylinositol 3-Kinase / Fibroblasts / Imidazoles Limits: Animals Language: Chinese Journal: Acta Academiae Medicinae Sinicae Year: 2013 Type: Article