Treatment of human brain tumor xenografts with O6-benzyl-2'-deoxyguanosine and BCNU.

  title={Treatment of human brain tumor xenografts with O6-benzyl-2'-deoxyguanosine and BCNU.},
  author={S. Clifford Schold and Demetrius M. Kokkinakis and Jack L Rudy and Robert C. Moschel and Anthony E. Pegg},
  journal={Cancer research},
  volume={56 9},
O6-Methylguanine-DNA methyltransferase (MGMT), a constitutively expressed DNA repair protein, removes alkyl groups from the O6-position of guanine in DNA. Tumor cells with high MGMT activity are resistant to nitrosoureas and other agents that form toxic O6-alkyl adducts. O6-Benzylguanine (BG) inactivates the MGMT protein and thereby enhances the sensitivity of tumor cells to alkylating drugs. However, the therapeutic potential of BG is limited by its poor solubility and its nonspecific… CONTINUE READING


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