Inhibition of topoisomerase I by heparin |
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| Authors: | K Ishii A Katase T Andoh N Seno |
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| Affiliation: | 1. Department of Hygienic Chemistry, Meiji College of Pharmacy, Yato 1-22-1 Tanashi, Tokyo 188, Japan;2. Department of Chemistry, Ochanomizu University, Ohtsuka 2-1-1, Bunkyo-ku, Tokyo 112, Japan |
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| Abstract: | DNA topoisomerase I isolated from mouse mammary cacinoma cells was shown to be inhibited by heparin, the dose giving 50% inhibition (IC50) being 0.20 μg/ml. Other chemically related acid mucopolysaccharides including heparan sulfate, dermatan sulfate etc. were more than 500 times less active than heparin. When the amount of enzyme was doubled relative to the substrate the inhibition was reversed. Addition of heparin to assay mixtures after the initiation of the reaction immediately inhibited the enzyme reaction. |
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| Keywords: | Please address correspondence to Dr. Andoh. |
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