Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

O6-B-dG (2R,3S,5R)-5-(2-amino-6- phenylmethoxy...

Synonyms: CHEMBL244316, SureCN6016114, AC1L2OIE, FT-0662724, 129732-90-7, ...

Wei, G. et al., Kokkinakis, D.M. et al.

Kokkinakis, Ahmed, Chendil, Moschel, Pegg,

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High impact information on O6-B-dG

Tumor-bearing mice were treated: (a) with a single i.p. injection of BCNU or TMZ at the maximum-tolerated doses of 75 and 340 mg/m(2), respectively; and (b) with O(6)-benzylguanine (BG) or O(6)-benzyl-2'-deoxyguanosine (dBG) in combination with BCNU or TMZ [1].
The prodrugs were found to be quite stable at physiological pH and were more than 200-fold less active as inactivators of O(6)-alkylguanine-DNA alkyltransferase (alkyltransferase) than either O(6)-benzylguanine or O(6)-benzyl-2'-deoxyguanosine [2].
However, as expected, incubation of these prodrugs with beta-glucuronidase in the culture medium led to much more efficient cell killing by BCNU as a result of the liberation of the more potent inactivators, O(6)-benzylguanine and O(6)-benzyl-2'-deoxyguanosine [2].

References

Sensitization of pancreatic tumor xenografts to carmustine and temozolomide by inactivation of their O6-Methylguanine-DNA methyltransferase with O6-benzylguanine or O6-benzyl-2'-deoxyguanosine. Kokkinakis, D.M., Ahmed, M.M., Chendil, D., Moschel, R.C., Pegg, A.E. Clin. Cancer Res. (2003) [Pubmed]
Beta-glucuronidase-cleavable prodrugs of O6-benzylguanine and O6-benzyl-2'-deoxyguanosine. Wei, G., Loktionova, N.A., Pegg, A.E., Moschel, R.C. J. Med. Chem. (2005) [Pubmed]

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