A New Cytotoxic Epothilone from Modified Polyketide Synthases Heterologously Expressed in Myxococcus xanthus

Autor: Arslanian, R. L., Tang, L., Blough, S., Ma, W., Qiu, R.-G., Katz, L., Carney, J. R.
Zdroj: Journal of Natural Products; July 2002, Vol. 65 Issue: 7 p1061-1064, 4p
Abstrakt: A new epothilone, 10,11-didehydroepothilone D (5), was isolated from a strain of the heterologous host Myxococcus xanthus genetically engineered to produce epothilone D (4). The structure of 5 was determined from NMR and MS data. The epothilone polyketide synthase was further modified in a recombinant M. xanthus strain to produce 5 as the major epothilone-related metabolite. The cytotoxicity of 5 against a panel of tumor cell lines, including several with multidrug resistance, and its effect on tubulin polymerization were comparable to epothilone D (4).
Databáze: Supplemental Index