Expanded Gene Targeting in RNA Hacking With G‐Tract‐Supply Staple Oligomers

T Tomoki Kida (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) Y Yua Hasegawa (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) M Miko Kato (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) M Mahiro Ohtani (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) A Ayu Matsumoto (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) R Ririka Taniguchi (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) R Rinka Ohno (Graduate School of Science and Technology Hirosaki University Hirosaki Aomori Japan) H Hiroshi Sugiyama (Institute For Integrated Cell‐Material Sciences (WPI‐iCeMS) Kyoto University Sakyo‐Ku Kyoto Japan) T Toshihiro Ihara (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) M Masaki Hagihara (Graduate School of Science and Technology Hirosaki University Hirosaki Aomori Japan) S Shin‐ichi Sato (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan) Y Yousuke Katsuda (Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan)

Abstract

ABSTRACT RNA hacking (RNAh) is a gene regulation technology that employs a short oligonucleotide, termed a Staple oligomer, to induce the formation of RNA G‐quadruplex structures on target mRNAs. While RNAh has the potential to target approximately 65% of human mRNAs, its applicability to the remaining genes is restricted by the sequence constraints. Herein, we present the G‐tract‐supply Staple oligomer (Gs‐Staple oligomer), designed to expand the range of targetable mRNAs within the RNAh framework. Incorporating G‐tracts into Staple oligomers alleviates the sequence constraints, enabling access to a broader range of mRNA targets. Gs‐Staple oligomers effectively suppressed the translation of target proteins in mammalian cells and in vivo. Furthermore, the gene suppression could be precisely modulated by adjusting the linker length between the G‐tracts. These findings have significantly expanded the versatility of RNAh, suggesting its potential for further development while highlighting its potential to be utilized as a nucleic acid‐based tool for research and clinical medicine.

Article Details

Volume / Issue Vol. 65, Issue 24
Published June 08, 2026
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (12)

T

Tomoki Kida

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

Y

Yua Hasegawa

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

M

Miko Kato

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

M

Mahiro Ohtani

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

A

Ayu Matsumoto

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

R

Ririka Taniguchi

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

R

Rinka Ohno

Graduate School of Science and Technology Hirosaki University Hirosaki Aomori Japan

H

Hiroshi Sugiyama

Institute For Integrated Cell‐Material Sciences (WPI‐iCeMS) Kyoto University Sakyo‐Ku Kyoto Japan

T

Toshihiro Ihara

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

M

Masaki Hagihara

Graduate School of Science and Technology Hirosaki University Hirosaki Aomori Japan

S

Shin‐ichi Sato

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan

Y

Yousuke Katsuda

Division of Materials Science and Chemistry Faculty of Advanced Science and Technology Kumamoto University Kumamoto Japan