Acta Academiae Medicinae Sinica

Acta Academiae Medicinae Sinica

Acta Academiae Medicinae Sinica ›› 2013, Vol. 35 ›› Issue (5): 530-534.doi: 10.3881/j.issn.1000-503X.2013.05.009

• Original Articles • Previous Articles     Next Articles

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

CHEN Xin-xin1,ZHANG Shu2,SHI Yu-zhuo1   

  1. 1 Department of Physiology,Institute of Basic Medical Sciences,CAMS and PUMC,Beijing 100005,China;
    2 Department of Dermatology,PUMC Hospital,CAMS and PUMC,Beijing 100730,China
  • Received:2013-05-08 Online:2013-11-01 Published:2013-11-01
  • Contact: CHEN Xin-xin Tel:010-69156468,
  • Supported by:

    Supported by the National Natural Sciences Foundation of China(81101516)


Objective 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.Methods 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.Results 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.Conclusion BEZ235 and U0126 are not suitable for a combined target therapy regimen.

Key words: receptor tyrosine kinase/phosphatidyl inositol-3-kinase/protein kinase B/mammalian target of rapamycin pathway, extracellular regulated protein kinase/mitogen-activated protein kinase pathway, BEZ235, U0126