Gifu University

Japan Science and Technology Agency

Wako Pure Chemical Industries, Inc.

Kitade, Yukio

Yukio Kitade

Yoshihito Ueno

Yoshiaki Kitamura

Aya Shibata

Remi Nakashima

The oligonucleotide derivative of the present invention is represented by Formula (1). This derivative is considered to be introduced into cells by binding of its amino sugar chain moiety to a ligand on cell surfaces, and have selective drug delivery function. The oligonucleotide derivative can be easily synthesized and introduced into cells without using a lipofection reagent. wherein A and B are independently modified or unmodified oligonucleotides whose total chain length is 3 or more, and A and B do not contain hydroxyl groups at 3' and 5&#x2032; ends of the oligonucleotide; S represents a sugar substituent, a peptide chain, or a tocopherol-binding group; and an alkyl group may be bound instead of hydrogen bound to a benzene ring.

Oligonucleotide derivative, oligonucleotide construct using the same, and methods for producing them

Provided is an RNA interference agent, with which a suppression effect on the off-target effect can be obtained with a simple system. The disclosures relate to an RNA interference agent provided with a single-stranded oligonucleotide passenger strand having one or two or more PAZ domain low-affinity units at the 3'-end.

RNA interference agent, method for producing same, and use therefor

The present invention provides an oligonucleotide derivative that enables to easily synthesize an oligonucleotide derivative chemically modified at the 3'-end with two moieties each having a benzene or pyridine structure with a few steps, an aromatic compound serving as a precursor for preparing the modification carrier for synthesizing oligonucleotide derivative, and the oligonucleotide derivative and the oligonucleotide construct using the same, that is chemically modified at the 3&#x2032;-end with two moieties each having a benzene or pyridine structure, and has good permeability through a cell membrane and excellent nuclease resistance. The modification carrier for synthesizing oligonucleotide derivative, comprising a unit and a carrier carrying the unit directly or via a linker, wherein the unit is represented by the formula (a): wherein, Rto Reach independently represent hydrogen or a substituent other than hydrogen; Zand Zeach independently represent CH or nitrogen; and X represents oxygen or sulfur. 

Oligonucleotide derivative comprising an aromatic compound

Provided is a nucleoside derivative which has a high affinity for RNA. Use is made of a nucleoside derivative represented by either formula (1) or formula (2). (In formulae (1) and (2), Z represents a carbon atom or a nitrogen atom; Rrepresents a hydrogen atom or a hydroxyl-protecting group; and Rrepresents a hydrogen atom or a phosphodiester group). 

RNA-selective hybridization reagent and use of the same

A labeling agent comprising a plurality of nucleotide derivative units represented by Formula (1) below: (where, Z represents a nitrogen atom or CH, Y represents an uncondensed aromatic hydrocarbon group or condensed polycyclic hydrocarbon group, Xrepresents O, S or Se, and Xrepresents SH (or S), Se, a Calkyl or a morpholino group).

Oligonucleotide derivative, labeling agent and use for labeling agent

The invention provides a 5'-amino-2&#x2032;-fluoro-2&#x2032;,5&#x2032;-dideoxynucleoside compound represented by the formula [1]: wherein Rrepresents a nucleic acid base which may have a protecting group; Rrepresents a hydrogen atom or an amino protecting group; and Rrepresents a hydrogen atom or a hydroxyl protecting group. The invention also provides a dideoxynucleoside-insoluble carrier bound substance and an oligonucleotide analogue involving the dideoxynucleoside compound.

Growing community of inventors

Gifu, Japan

Yukio Kitade