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2016 Fiscal Year Final Research Report

Development of CpG island binding molecule based on artificial dinucleotide

Research Project

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Project/Area Number 26670056
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionKyushu University

Principal Investigator

Taniguchi Yosuke  九州大学, 薬学研究院, 准教授 (00452714)

Project Period (FY) 2014-04-01 – 2017-03-31
Keywords核酸医薬 / 核酸化学 / 分子認識 / 人工核酸
Outline of Final Research Achievements

In this study, we tried to create novel artificial molecules capable of binding to CpG islands deeply involved in the epigenetic regulation mechanism of gene expression. Focusing on the G/GC base triplet structure of natural type triplex DNA formation, an artificial nucleic acid analogue having an aromatic ring at the 2-position of guanosine was designed as a recognition molecule. We have succeeded in chemical synthesis of the target compound. After incorporation of them into oligonucleotide using an automated DNA synthesizer, we evaluated the interaction with duplex DNA and synthesized oligonucleotides. We found that the artificial nucleic acid containing benzene ring could recognize the GC base pair with high stability and selectivity by comparing the association constant of the natural type guanosine. Moreover, we succeeded in finding that it has recognition ability if only one is contained regardless of where it is incorporated in the oligonucleotide.

Free Research Field

核酸化学

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Published: 2018-03-22  

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