Kyowa Hakko Kirin Co., Limited

Kyowa Kirin Co., Ltd.

Fumikazu Shinohara

Yuichi Takahashi

Tomoyuki Nishikawa

Michihiko Suzuki

Takahiro Nakajima

Junichiro Yamamoto

Masakazu Homma

Jun-ichi Saito

Asana Makino

Masayoshi Nakoji

Taiji Oashi

Toshimasa Harumoto

Yasuo Kouda

Kenji Hagiwara

An oligonucleotide having improved affinity for AGO2 is disclosed. The oligonucleotide has a nucleotide residue or a nucleoside residue represented by formula (I) wherein Xis an oxygen atom or the like, Ris formula (IIA), wherein Ris halogen or the like, and Ris a hydrogen atom or the like, or formula (IVA) wherein Yis a nitrogen atom or the like, and Yis CH or the like, or the like, Ris a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and Ris a hydrogen atom or the like at the 5' end thereof, and the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3. A method for improving the knockdown activity of an oligonucleotide wherein the oligonucleotide has a knockdown activity against an mRNA encoding a protein involved in a disease. 

Oligonucleotide

An oligonucleotide having a nucleotide residue or a nucleoside residue represented by formula (I) {wherein Xis an oxygen atom or the like, Ris formula (IIA) (wherein Ris halogen or the like, and Ris a hydrogen atom or the like), formula (IVA) (wherein Yis a nitrogen atom or the like, and Yis CH or the like), or the like, Ris a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and Ris a hydrogen atom or the like, or formula (VI) (wherein n2 is 1, 2 or 3)} at the 5' end thereof, wherein the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3, is provided. 

Oligonucleotide having non-natural nucleotide at 5'-terminal thereof

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Tokyo, Japan

Fumikazu Shinohara