Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions

Go Hirai; Megumi Ohkubo; Yuki Tamura; Mikiko Sodeoka

doi:10.1016/j.bmcl.2011.04.108

Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3587-90. doi: 10.1016/j.bmcl.2011.04.108. Epub 2011 Apr 28.

Authors

Go Hirai¹, Megumi Ohkubo, Yuki Tamura, Mikiko Sodeoka

Affiliation

¹ RIKEN Advanced Science Institute, Hirosawa, Wako, Japan.

PMID: 21596562
DOI: 10.1016/j.bmcl.2011.04.108

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

Enzyme Activators
Phorbol Esters
Protein Kinase C-alpha