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Belizeanic acid: a potent protein phosphatase 1 inhibitor belonging to the okadaic acid class, with an unusual skeleton.

  作者 Cruz, Patricia G.;Fernandez, Jose Javier;Norte, Manuel;Daranas, Antonio Hernandez;  
  选自 期刊  Chemistry-A European Journal;  卷期  2008年14-23;  页码  6948-6956  
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[摘要]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 behavior of BA was elucidated by a combination of NMR spectroscopy and conformational anal. 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 compds. 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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