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.

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Bibliographic Details
Main Authors: Cruz, Patricia G., Fernández, José J., Norte, Manuel, Hernández Daranas, Antonio
Other Authors: Ministerio de Educación y Ciencia (España)
Format: artículo biblioteca
Language:English
Published: Wiley-VCH 2008-08-08
Subjects:Biosynthesis, Conformation analysis, Enzyme inhibitors, Natural products, Structure elucidation,
Online Access:http://hdl.handle.net/10261/213347
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