Development and application of a novel screening technolgy toward effective uses of chemical library

2014 Fiscal Year Final Research Report

• Project/Area Number: 24659046
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Drug development chemistry
• Research Institution: Kyoto University
• Principal Investigator: FUJII Nobutaka 京都大学, 薬学研究科(研究院), 教授 (60109014)
• Co-Investigator(Renkei-kenkyūsha): OHNO Hiroaki 京都大学, 大学院薬学研究科, 教授 (30322192) ; OISHI Shinya 京都大学, 大学院薬学研究科, 講師 (80381739)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: 天然物 / 化合物ライブラリー / スクリーニング / アッセイ / 生物活性化合物 / 鏡像体

Outline of Final Research Achievements

Development of a novel screening approach was achieved toward effective uses of chiral compound libraries for drug discovery. Two cancer-related proteins (MDM2, MDMX) with the native structures and functions were prepared via a standard solid-phase peptide synthesis and appropriate folding conditions. Using these synthetic proteins for screening of in-house chemical library and natural product library, a number of hit compounds were identified via a primary chemical array-mediated screening and the subsequent fluorescence polarization assay.

Free Research Field

創薬化学