Abstract
Peloruside A is a novel secondary metabolite isolated from a New Zealand marine sponge, Mycale hentscheli, that has potent paclitaxel-like microtubule-stabilizing activity and is cytotoxic at nanomolar concentrations. Its 16-membered macrolide ring is similar to that of epothilone, a drug currently under clinical investigation as an anticancer agent. Like paclitaxel, peloruside A arrests cells in the G(2)-M phase of the cell cycle and induces apoptosis. The relatively simple structure of peloruside makes it suitable for the design and synthesis of analogues with improved tumor targeting and reduced tumor cross-resistance.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Actins / metabolism
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Adenocarcinoma / drug therapy
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Adenocarcinoma / metabolism
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Adenocarcinoma / pathology
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Bridged Bicyclo Compounds, Heterocyclic / chemistry
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
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Cell Cycle / drug effects
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Epothilones*
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Humans
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Lactones / chemistry
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Lactones / pharmacology*
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Lung Neoplasms / drug therapy
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Lung Neoplasms / metabolism
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Lung Neoplasms / pathology
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Macrolides / chemistry
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Macrolides / pharmacology
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Microtubules / drug effects
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Paclitaxel / analogs & derivatives*
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Paclitaxel / chemistry
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Paclitaxel / pharmacology
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Taxoids*
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Tubulin / metabolism
Substances
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Actins
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Antineoplastic Agents
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Bridged Bicyclo Compounds, Heterocyclic
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Epothilones
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Lactones
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Macrolides
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Taxoids
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Tubulin
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laulimalide
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peloruside A
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Paclitaxel
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epothilone B