Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba.

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Suzuki K, Yahara S, Maehata K, Uyeda M

Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba.

J Nat Prod. 2001 Feb;64(2):204-7.

PubMed ID
11430001 [ View in PubMed
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Abstract

A novel inhibitor of topoisomerase I designated as isoaurostatin (1) was isolated from the culture filtrate of Thermomonospora alba strain No. 1520. The structure of 1 was determined to be 6,4'-dihydroxyisoaurone on the basis of spectroscopic (NMR and MS) methods. Compound 1 inhibited the relaxation activity of calf thymus topoisomerase I in a noncompetitive manner and did not inhibit the relaxation and decatenation of human placenta topoisomerase II. Compound 1 is an inhibitor belonging to cleavable complex-nonforming type without DNA intercalation.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CamptothecinDNA topoisomerase 1IC 50 (nM)4000N/AN/ADetails
CamptothecinDNA topoisomerase 1IC 50 (nM)17000N/AN/ADetails
CamptothecinDNA topoisomerase 1IC 50 (nM)9000N/AN/ADetails
DoxorubicinDNA topoisomerase 2-alphaIC 50 (nM)1000N/AN/ADetails