Article
Human small cell lung cancer NYH cells resistant to the bisdioxopiperazine ICRF-187 exhibit a functional dominant Tyr165Ser mutation in the Walker A ATP binding site of topoisomerase II alpha.
FEBS letters - 5 Jun 2002
Wessel Irene, Jensen Lars H, Renodon-Corniere Axelle, Sorensen Tina K, Nitiss John L, Jensen Peter B, Sehested Maxwell
Abstract excerpt
Bisdioxopiperazine anti-cancer agents are catalytic inhibitors of topoisomerase II which by unknown means lock the enzyme in a closed clamp form and inhibit its ATPase activity. In order to demarcate a putative pharmacophore, we here describe a novel Tyr165Ser mutation in the enzyme's Walker A ATP binding site leading to specific bisdioxopiperazine resistance when transformed into a temperature-conditional yeast...
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