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O6-Benzylguanine


O6-Benzylguanine (O6-BG) is a synthetic derivative of guanine. It is an antineoplastic agent. It exerts its effect by acting as a suicide inhibitor of the enzyme O6-alkylguanine-DNA alkyltransferase which leads to interruption of DNA repair. O6-BG was used clinically in combination with the alkylating agent temozolomide for glioblastoma, however the combination was found to be overly toxic without adding significant benefit.

O6-BG is also used as a biochemical tool in the study of DNA repair mechanisms.

References

References

  1. (2005). "Phase I trial of temozolomide plus O6-benzylguanine for patients with recurrent or progressive malignant glioma". Journal of Clinical Oncology.
  2. (2009). "Phase II Trial of Temozolomide Plus O6-Benzylguanine in Adults with Recurrent, Temozolomide-Resistant Malignant Glioma". Journal of Clinical Oncology.
  3. Blumenthal, Deborah T.. (2015). "A phase III study of radiation therapy (RT) and O6-benzylguanine, (O6-BG) plus BCNU versus RT and BCNU alone and methylation status in newly-diagnosed glioblastoma (GBM) and gliosarcoma: Southwest Oncology Group (SWOG) Study S0001". International Journal of Clinical Oncology.
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