EFFECT OF SOME NONINTERCALATIVE ANTITUMOR DRUGS ON THE ACTIVITY OF CALF THYMUS DNA TOPOISOMERASE Ⅰ
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Abstract
DNA topoisomerase Ⅰ has been isolated from the nuclei of calf thymus by PEG fractionation and chromatography on P11 and on Bio-Rex 70. Either a positive or negative suPercoiled pBR322 DNA can be relaxed by the enzyme. The activity of Topo Ⅰ is Mg2+ and ATP independent. Some of nonintercalative antitumor drugs such as camptothecine, hydroxycamptothecine, cyclophosphamide, methotrexate and mitomycin C were found to inhibitthe activity of Tdpo Ⅰ. The results suggest that DNA Topo Ⅰ can be used to screen new nonintercalative antitumor drugs as a target protein.
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