Carteriosulfonic acids A-C, GSK-3beta inhibitors from a Carteriospongia sp.

Carteriosulfonic acids A-C, GSK-3beta inhibitors from a Carteriospongia sp.
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DOI:
10.1021/np900336f
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发表时间:
2009-09
影响因子:
5.1
通讯作者:
Ireland, Chris M.
Ireland, Chris M.
中科院分区:
生物学2区
文献类型:
--
作者:
McCulloch, Malcolm W. B.;Bugni, Tim S.;Concepcion, Gisela P.;Coombs, Gary S.;Harper, Mary Kay;Kaur, Simran;Mangalindan, Gina C.;Mutizwa, Misha M.;Veltri, Charles A.;Virshup, David M.;Ireland, Chris M.

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Modulators of Wnt signaling have therapeutic potential in a number of human diseases. A fractionated library from marine invertebrates was screened in a luciferase assay designed to identify modulators of Wnt signaling. A fraction from a Carteriospongia sp. sponge activated Wnt signaling and was subsequently shown to inhibit GSK-3β, which inhibits Wnt signaling through phosphorylation of β-catenin. Three novel natural products, carteriosulfonic acids A (1), B (2) and C (3), were identified as active constituents. The carteriosulfonic acids contain unprecedented 4,6,7,9-tetrahydroxylated decanoic acid subunits. Their structures were elucidated through analysis of NMR data and a detailed analysis of pseudo MS3 spectra.
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