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Topoisomerase II: A potential target for novel antifungal agents

Figgitt, D. P., Denyer, Stephen Paul, Dewick, P. M., Jackson, D. E. and Williams, P. 1989. Topoisomerase II: A potential target for novel antifungal agents. Biochemical and Biophysical Research Communications 160 (1) , pp. 257-262. 10.1016/0006-291X(89)91649-5

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Several podophyllotoxin-related lignans have been shown to possess significant antifungal activity against a number of filamentous fungi. Initial structure-activity studies indicate this action is sensitive to change at the 4 and 4′ positions of the podophyllotoxin skeleton. Good correlation has been observed between antifungal action and the ability to inhibit the relaxation of supercoiled plasmid DNA by a topoisomerase II preparation from Saccharomyces cerevisiae. Etoposide, an inhibitor of mammalian topoisomerase II, is inactive against this yeast enzyme, although good inhibition is shown by amiloride, 4′-(9-acridinylamino)-methanesulphon-m-anisidide (m-AMSA) and novobiocin, known inhibitors of the mammalian enzyme.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RM Therapeutics. Pharmacology
Publisher: Elsevier
ISSN: 0006-291X
Last Modified: 19 Mar 2016 23:14

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