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dc.contributor.authorField, Jessica J.-
dc.contributor.authorNorthcote, Peter-
dc.contributor.authorPaterson, Ian-
dc.contributor.authorAltmann, Karl-Heinz-
dc.contributor.authorDíaz, José Fernando-
dc.contributor.authorMiller, John H.-
dc.identifierdoi: 10.3390/ijms18050971-
dc.identifier.citationInternational Journal of Molecular Sciences 18 (5): 971 (2017)-
dc.description.abstractZampanolide, first discovered in a sponge extract in 1996 and later identified as a microtubule-stabilizing agent in 2009, is a covalent binding secondary metabolite with potent, low nanomolar activity in mammalian cells. Zampanolide was not susceptible to single amino acid mutations at the taxoid site of β-tubulin in human ovarian cancer 1A9 cells, despite evidence that it selectively binds to the taxoid site. As expected, it did not synergize with other taxoid site microtubule-stabilizing agents (paclitaxel, ixabepilone, discodermolide), but surprisingly also did not synergize in 1A9 cells with laulimalide/peloruside binding site agents either. Efforts to generate a zampanolide-resistant cell line were unsuccessful. Using a standard wound scratch assay in cell culture, it was an effective inhibitor of migration of human umbilical vein endothelial cells (HUVEC) and fibroblast cells (D551). These properties of covalent binding, the ability to inhibit cell growth in paclitaxel and epothilone resistant cells, and the ability to inhibit cell migration suggest that it would be of interest to investigate zampanolide in preclinical animal models to determine if it is effective in vivo at preventing tumor growth and metastasis.-
dc.description.sponsorship: The authors thank the Cancer Society of New Zealand, Wellington Medical Research Foundation, and Victoria University for support of the project (Jessica J. Field & John H. Miller). Jessica J. Field was a recipient of a Joy McNicholl research scholarship. The authors also thank Ariane Chan and Craig Doney of Victoria University for designing and making available the wound scratch assay plate insert. We thank Arun Kanakkanthara for providing some of the IC50 values for the LAU treatment of 1A9-L4 cells in Table 3.-
dc.description.sponsorshipWe acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI).-
dc.publisherMultidisciplinary Digital Publishing Institute-
dc.relation.isversionofPublisher's version-
dc.titleZampanolide, a Microtubule-Stabilizing Agent, Is Active in Resistant Cancer Cells and Inhibits Cell Migration-
dc.contributor.funderConsejo Superior de Investigaciones Científicas (España)-
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