Selective detection and stabilization of G-quadruplexes in genome using G4 ligands

2017 Fiscal Year Final Research Report

• Project/Area Number: 26282214
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Partial Multi-year Fund
• Section: 一般
• Research Field: Chemical biology
• Research Institution: Tokyo University of Agriculture and Technology
• Principal Investigator: Nagasawa Kazuo 東京農工大学, 工学(系)研究科(研究院), 教授 (10247223)
• Project Period (FY): 2014-04-01 – 2018-03-31
• Keywords: グアニン四重鎖 / テロメア / 大環状ポリオキサゾール / ビオチンプローブ / G４アフィニティカラム / トポロジー

Outline of Final Research Achievements

G-quadruplex (G4), a higher order structure of DNA, is involved in transcriptional regulation of genes, and detection of G4s in genome leads to the discoveries of new drug targets. Furthermore, selective stabilization of each G4 would become the selective control of the corresponding G4 function. Based on our macrocyclic polyoxazole type G4 ligand (6OTD, 7OTD), we have developed a new 7OTD analog attached with biotin-function. With the new ligand, we prepared a G4 affinity column, which enable us to detect the G4-forming DNA sequences in genome. In addition, we have developed new 6OTD derivatives for stabilizing two out of three representative topologies in G4 selectively.

Free Research Field

有機合成化学