Discovery of ubiquitin-activating enzyme inhibitors designed based on its catalytic mechanism

2016 Fiscal Year Final Research Report

• Project/Area Number: 26870495
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Chemical pharmacy; Drug development chemistry
• Research Institution: Kyoto Prefectural University of Medicine
• Principal Investigator: Itoh Yukihiro 京都府立医科大学, 医学(系)研究科(研究院), 講師 (30636402)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: ドラッグデザイン / 低分子薬物 / 触媒メカニズム

Outline of Final Research Achievements

It has been reported that ubiquitin-activating enzyme is highly expressed in leukemic cells and that inhibition of the enzyme disturbs their proliferation.
Therefore, ubiquitin-activating enzymes are interesting as a drug target. In this study, we attempted to discover ubiquitin-activating enzyme inhibitors. Based on the catalytic mechanism of ubiquitin-activating enzyme, we designed and synthesized several compounds which were expected to show inhibitory activity dependent on enzyme reaction. As a result of their biological evaluation, we succeeded in identification of a compound inhibiting ubiquitin-activing enzyme.

Free Research Field

創薬化学