Kyowa Hakko Kirin Co., Limited

Kyowa Kirin Co., Ltd.

Asana Makino

Yuichi Takahashi

Tomoyuki Nishikawa

Michihiko Suzuki

Takahiro Nakajima

Junichiro Yamamoto

Jun-ichi Saito

Masayoshi Nakoji

Fumikazu Shinohara

Taiji Oashi

Yasuhiro Suzuki

Keiji Uehara

Hiroto Iwai

Toshimasa Harumoto

Yasuo Kouda

The present invention provides a nucleic acid conjugate in which a sugar chain ligand is bonded to an oligonucleotide via a linker, the sugar chain ligand having O-bonded mannose at its non-reducing end.

Nucleic acid conjugate

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

Asana Makino