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2016 Fiscal Year Final Research Report

Development of SIRT6 activators targeting for Warburg effect

Research Project

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Project/Area Number 15K18899
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionNagoya City University

Principal Investigator

Kawaguchi Mitsuyasu  名古屋市立大学, 大学院薬学研究科, 助教 (10735682)

Project Period (FY) 2015-04-01 – 2017-03-31
KeywordsSirtuin / 蛍光プローブ
Outline of Final Research Achievements

In general, sirtuin activity is detectable by a protease (eg. trypsin) coupled two-steps method. However, such method has several problems, cumbersome procedure, false-positive compounds on chemical screening.
In this study, focusing on interesting reports showing that sirtuin recognize and hydrolize long-chain fatty acyl groups, we hypothesized that sirtuin can hydrolize acyl groups of large quencher dyes. We exhibited that sirtuin activity is detectable by a FRET based novel fluorescence probe, SFP3, and applied this methodology for chemical screening. We identified novel scaffolds of SIRT6 inhibitor and activiator.

Free Research Field

ケミカルバイオロジー

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Published: 2018-03-22  

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