Belizeanic Acid: A Potent Protein Phosphatase 1 Inhibitor Belonging to the Okadaic Acid Class, with an Unusual Skeleton
Belizeanic acid (BA), a novel metabolite belonging to the okadaic acid class of protein phosphatase inhibitors, was isolated from artificial cultures of the dinoflagellate Prorocentrum belizeanum . The structure and conformational behaviour of BA was elucidated by a combination of NMR spectroscopy and conformational analysis. The isolation of this metabolite, which possesses a simplified version of the okadaic acid skeleton, supports the biogenetic pathway previously reported for this class of compounds. BA showed potent inhibitory activity against protein phosphatase 1 (PP1) within the nM range. A plausible model for the interaction of BA with the PP1 binding pocket was derived from computational docking studies.
Main Authors: | , , , |
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Other Authors: | |
Format: | artículo biblioteca |
Language: | English |
Published: |
Wiley-VCH
2008-08-08
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Subjects: | Biosynthesis, Conformation analysis, Enzyme inhibitors, Natural products, Structure elucidation, |
Online Access: | http://hdl.handle.net/10261/213347 |
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Summary: | Belizeanic acid (BA), a novel metabolite belonging to the okadaic acid class of protein phosphatase inhibitors, was isolated from artificial cultures of the dinoflagellate Prorocentrum belizeanum . The structure and conformational behaviour of BA was elucidated by a combination of NMR spectroscopy and conformational analysis. The isolation of this metabolite, which possesses a simplified version of the okadaic acid skeleton, supports the biogenetic pathway previously reported for this class of compounds. BA showed potent inhibitory activity against protein phosphatase 1 (PP1) within the nM range. A plausible model for the interaction of BA with the PP1 binding pocket was derived from computational docking studies. |
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