Dna binding agents

A splicing factor SF2/ASF is a natural substrate for the kinase activity of human topoisomerase I. This study demonstrates that SF2/ASF inhibits DNA cleavage by human topoisomerase I induced by the anti-cancer agent camptothecin. The inhibition is independent of the phosphorylation status of SF2/ASF. We show that the inhibition did not result from binding of SF2/ASF to DNA that would hinder interactions between topoisomerase I and DNA. Neither it was a consequence of a loss of sensitivity of the enzyme to camptothecin.

7p research12 01-06-2013 39 5   Download

The benzoacronycine derivative, S23906-1, was character-ized recently as a novel potent antitumor agent through alkylation of theN2 positionof guanines inDNA.We show here that its reactivity towards DNA can be modulated by glutathione (GSH). The formation of covalent adducts between GSH and S23906-1 was evidenced by EI-MS, and the use of different GSH derivatives, amino acids and dipeptides revealed that the cysteine thiol group is absolutely required for complex formation because glutathione disul-fide (GSSG) and other S-blocked derivatives failed to react covalently with S23906-1. ...

12p fptmusic 16-04-2013 41 4   Download