Inhibition of human DNA polymerase β activity by the anticancer prodrug Cloretazine

The antineoplastic prodrug Cloretazine exerts its cytotoxicity via a synergism between 2-chloroethylating and carbamoylating activities that are cogenerated upon activation in situ. Cloretazine is reported here to inhibit the nucleotidyl-transferase activity of purified human DNA polymerase β (Pol β...

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Veröffentlicht in:	Biochemical and biophysical research communications 2009-01, Vol.378 (3), p.419-423
Hauptverfasser:	Frederick, Abbie M., Davis, Marguerite L., Rice, Kevin P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - pharmacology Carbamoylation Cloretazine DNA alkylation DNA base excision repair DNA crosslinking agents DNA polymerase beta DNA Polymerase beta - antagonists & inhibitors DNA Polymerase I - antagonists & inhibitors DNA Repair - drug effects Humans Hydrazines - pharmacology Inhibitory Concentration 50 Methyl isocyanate Prodrugs - pharmacology Sulfonamides - pharmacology
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