O6-Benzylguanine Explained

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.^{[1] [2] [3]}

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

External links

• Can O6-alkylguanine-DNA alkyltransferase depletion enhance alkylator activity in the clinic? . 10955771 . 2000 . Friedman . HS . 6 . 8 . 2967–8 . Clinical Cancer Research .

Notes and References

1. 16192602 . 2005 . Quinn . JA . Desjardins . A . Weingart . J . Brem . H . Dolan . ME . Delaney . SM . Vredenburgh . J . Rich . J . Friedman . AH . Reardon . D. A. . Sampson . J. H. . Pegg . A. E. . Moschel . R. C. . Birch . R . McLendon . R. E. . Provenzale . J. M. . Gururangan . S . Dancey . J. E. . Maxwell . J . Tourt-Uhlig . S . Herndon Je . 2nd . Bigner . D. D. . Friedman . H. S. . Phase I trial of temozolomide plus O6-benzylguanine for patients with recurrent or progressive malignant glioma . 23 . 28 . 7178–87 . 10.1200/JCO.2005.06.502 . Journal of Clinical Oncology. 8 . free .
2. 10.1200/JCO.2008.18.8417 . Phase II Trial of Temozolomide Plus O6-Benzylguanine in Adults with Recurrent, Temozolomide-Resistant Malignant Glioma . 2009 . Quinn . J. A. . Jiang . S. X. . Reardon . D. A. . Desjardins . A. . Vredenburgh . J. J. . Rich . J. N. . Gururangan . S. . Friedman . A. H. . Bigner . D. D. . Sampson . J. H. . McLendon . R. E. . Herndon . J. E. . Walker . A. . Friedman . H. S. . Journal of Clinical Oncology . 27 . 8 . 1262–7 . 19204199 . 2667825. 8 .
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 . 10.1007/s10147-014-0769-0 . 4465052 . 25407559 . 20 . 4 . 650–8.