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Start Over Author "Ohkubo, Megumi" Topic drug design
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1. Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.

Author

Hirai G, Ohkubo M, Tamura Y, and Sodeoka M

Subjects
Animals, Binding Sites, Enzyme Activation drug effects, Enzyme Activators chemistry, Enzyme Activators pharmacology, Humans, Models, Biological, Molecular Structure, Phorbol Esters chemistry, Phorbol Esters metabolism, Protein Binding, Drug Design, Enzyme Activators chemical synthesis, Protein Kinase C-alpha metabolism
Abstract

Novel types of PKCα 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 PKCα, but their binding sites were not the same as that of phorbol ester., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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