Osaka University

National Institutes of Biomedical Innovation, Health and Nutrition

Kobe University

Tokyo Medical and Dental University

Aichi Medical University

Luxna Biotech Co., Ltd.

Yuya Kasahara

Satoshi Obika

Reiko Waki

Takao Inoue

Tokuyuki Yoshida

Kunihiko Morihiro

Atsushi Mikami

Takanori Yokota

Takao Suzuki

Hideki Mochizuki

Masayuki Nakamori

Takumi Fukumoto

Tetuya Nagata

Shinji Matsumoto

Akira Kikuchi

Kosei Takeuchi

Masahito Shimojo

Masaki Yamagami

Tadashi Umemoto

The present invention aims to provide an antisense oligonucleic acid with reduced hepatotoxicity. The antisense oligonucleic acid according to the present invention is characterized in that it has a base length of not less than 7 nt and not more than 30 nt, wherein nucleic acid residues of not less than 1 nt and not more than 5 nt respectively from the both terminals are 2',4′-bridged nucleic acids, 2′,4′-non-bridged nucleic acid residue(s) is(are) present between the above-mentioned both terminals, and one or more bases in the nucleic acid residue(s) of the above-mentioned 2′,4′-non-bridged nucleic acid residue(s) is/are modified.

Antisense oligonucleic acid

The purpose of the present invention is to provide an antisense oligonucleotide that targets an ARL4C molecule and exerts an antitumor effect in vivo, and a nucleic acid drug using the antisense oligonucleotide. An antisense oligonucleotide that has a base sequence consisting of at least 10 consecutive bases contained in the base sequence represented by SEQ ID NO: 1. This antisense oligonucleotide targets an ARL4C molecule and thus can inhibit the expression of ARL4C in a tumor cell in vitro and suppress the migration and proliferation thereof. When systemically administered, moreover, the antisense oligonucleotide can exert an excellent antitumor effect in vivo too.

Antisense oligonucleotide targeting ARL4C molecule, and nucleic acid drug using antisense oligonucleotide

Disclosed is an oligonucleotide or a pharmacologically acceptable salt thereof, wherein the oligonucleotide comprises at least one defined nucleoside structure, can bind to a human nSR100 gene and has human nSR100 expression inhibiting activity. The oligonucleotide has a length of 12 to 20 mer, and is complementary to a defined target region. Further, disclosed is an nSR100 gene expression inhibitor and a cancer therapeutic agent containing the oligonucleotide or the pharmacologically acceptable salt thereof. The cancer therapeutic agent is used for treatment of small cell lung cancer, prostate cancer, or breast cancer.

Small cell lung cancer therapeutic agent containing oligonucleotide

The present invention provides an antisense oligonucleotide for inhibiting biosynthesis of chondroitin sulfate. The antisense oligonucleotide comprises at least one modified nucleotide, wherein the antisense oligonucleotide suppresses expression of one or both of the chondroitin sulfate N-acetylgalactosaminyltransferase-1 (CSGalNAcT1) gene and the chondroitin sulfate N-acetylgalactosaminyltransferase-2 (CSGalNAcT2) gene.

Antisense nucleic acid for inhibiting biosynthesis of chondroitin sulfate

The present invention aims to provide an antisense oligonucleic acid with reduced hepatotoxicity. The antisense oligonucleic acid according to the present invention is characterized in that it has a base length of not less than 7 nt and not more than 30 nt, wherein nucleic acid residues of not less than 1 nt and not more than 5 nt respectively from the both terminals are 2',4&#x2032;-bridged nucleic acids, 2&#x2032;,4&#x2032;-non-bridged nucleic acid residue(s) is(are) present between the above-mentioned both terminals, and one or more bases in the nucleic acid residue(s) of the above-mentioned 2&#x2032;,4&#x2032;-non-bridged nucleic acid residue(s) is/are modified.

The present invention can provide a nucleic acid medicine which has a higher effect and a more prolonged effect of inhibiting the expression of &#x3b1;-synudein can be provided. Disclosed is the oligonucleotide or a pharmacologically acceptable salt thereof, the oligonucleotide containing at least one nucleoside structure represented by Formula (I): (where each of Base and A are defined substituent or structure), can bind to an &#x3b1;-synudein gene, has activity for inhibiting expression of the &#x3b1;-synudein gene, and is complementary to the &#x3b1;-synudein gene, and the oligonucleotide has a length of twelve to twenty bases. 

&#x3b1;-synuclein expression inhibitor

Growing community of inventors

Osaka, Japan

Yuya Kasahara