Generation of novel drug targeting protein kinase epsilon for type 2 diabetes mellitus.

2011 Fiscal Year Final Research Report

• Project/Area Number: 22710194
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Medical genome science
• Research Institution: 独立行政法人国立成育医療研究センター (2011); Tokai University (2010)
• Principal Investigator: YONEZAWA Tomo 独立行政法人国立成育医療研究センター, システム発生・再生医学研究部, 流動研究員 (60515964)
• Project Period (FY): 2010 – 2011
• Keywords: 2型糖尿病 / プロテインキナーゼCε(PKCε) / 新規治療薬 / トランスレーショナルリサーチ

Research Abstract

We identified the susceptible gene as a protein kinase C epsilon(PKCε) for type 2 diabetes mellitus via genome-wide association study using microsatellites, prompting us to generate the small molecule drug targeting PKCε. Our in silico strategy using over 60, 000 chemical library identified several potential compounds including drug X possibly affecting the activity of PKCε. We also validated the effect of them using molecular-and cell-based assay.