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Design And Synthesis Of Protein Kinase C Alpha Activators Based On 'Out Of Pocket' Interactions

Go Hirai,Megumi Ohkubo,Yuki Tamura,Mikiko Sodeoka

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2011）

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Abstract
Novel types of PKC alpha activators based on isobenzofuranone bearing a myo-inositol moiety were designed and synthesized. The derivatives with bulky substituents on the myo-inositol moiety significantly activated PKC alpha, but their binding sites were not the same as that of phorbol ester. (C) 2011 Elsevier Ltd. All rights reserved.
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Key words
Protein kinase C alpha,Isobenzofuranone derivatives,Enzymatic activity,myo-Inositol,Binding model
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