Article
Polar, functionalized guanine-O6 derivatives resistant to repair by O6-alkylguanine-DNA alkyltransferase: implications for the design of DNA-modifying drugs.
European journal of medicinal chemistry - 1 Mar 2006
Pletsas Dimitrios, Wheelhouse Richard T, Pletsa Vassiliki, Nicolaou Anna, Jenkins Terence C, Bibby Michael C, Kyrtopoulos Soterios A
Abstract excerpt
The protein O6-alkylguanine-DNA alkyltransferase (Atase) is responsible for the repair of DNA lesions generated by several clinically important anti-cancer drugs; this is manifest as active resistance in those cancer cell lines proficient in Atase expression. Novel O6-substituted guanine analogues have been synthesized, bearing acidic, basic and hydrogen bonding functional groups. In contrast to existing...
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