Bonac Corporation

Tomohiro Hamasaki

Tadaaki Ohgi

Hiroshi Suzuki

Hisao Shirohzu

Akihiro Itoh

Hirotake Hayashi

Eriko Aoki

Chisato Emura

Takayuki Mizutani

The invention provides a single-stranded nucleic acid capable of inhibiting expression of a target gene having a delivery function. The nucleic acid contains, from the 5'-side to the 3&#x2032;-side, a 5&#x2032;-side region (Xc), a linker region (Lx), an inner region (Z), a linker region (Ly) and a 3&#x2032;-side region (Yc) in this order, wherein the inner region (Z) is constituted by linkage of the inner 5&#x2032;-side region (X) and the inner 3&#x2032;-side region (Y), the 5&#x2032;-side region (Xc) is complementary to the inner 5&#x2032;-side region (X), the 3&#x2032;-side region (Yc) is complementary to the inner 3&#x2032;-side region (Y), at least one of the inner region (Z), the 5&#x2032;-side region (Xc) and the 3&#x2032;-side region (Yc) comprises an expression inhibitory sequence that inhibits expression of a target gene, and at least one of the 5&#x2032;-terminus, the 3&#x2032;-terminus, the linker region (Lx) and the linker region (Ly) is bound to a bio-related substance.

Single-stranded nucleic acid molecule for regulating expression of gene having delivering function

The invention provides a microRNA inhibitor that has two or more sequences complementary to the sequence of microRNA to be the target of inhibition, which two or more complementary sequences are linked via one or more linker residues.

Micro-RNA inhibitor

The invention provides a single-stranded nucleic acid molecule containing an expression inhibitory sequence that inhibits expression of a target gene, region (X), linker region (Lx), and region (Xc), wherein the linker region (Lx) is linked between the region (Xc) and the region (Xc), the region (Xc) is complementary to the region (X), at least one of the region (X) and the region (Xc) contains the expression inhibitory sequence, and the linker region (Lx) contains an atomic group derived from an amino acid. The single-stranded nucleic acid molecule can inhibit expression of the target gene.

Single-stranded nucleic acid molecule having amino acid backbone

Micro-RMA inhibitor

The present invention provides a process for preparing an isotope-containing phosphate compound easily. The process for preparing an isotope-containing phosphate compound according to the present invention includes the step of: oxidizing a trivalent phosphorus compound with an oxidizing agent containing an isotope to synthesize a pentavalent phosphate compound to which the isotope has been introduced. The present invention preferably is applied to the synthesis of nucleic acids such as DNA and RNA, for example. The isotope preferably is a stable isotope. The oxidizing agent preferably is HO, 3H-1,2-benzodithiol 3-one 1,1-dioxide havingS, or a diisopropylethylamine-borane complex havingB, for example.

Process for preparing phosphate compound bearing isotope

Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.

Single-stranded nucleic acid molecule having nitrogen-containing alicyclic skeleton

Provided is a novel nucleic acid molecule that is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes, in sequence from the 5' side to the 3&#x2032; side: a 5&#x2032; side region (Xc); an inner region (Z); and a 3&#x2032; side region (Yc). The inner region (Z) is composed of an inner 5&#x2032; side region (X) and an inner 3&#x2032; side region (Y) that are linked to each other. The 5&#x2032; side region (Xc) is complementary to the inner 5&#x2032; side region (X). The 3&#x2032; side region (Yc) is complementary to the inner 3&#x2032; side region (Y). At least one of the inner region (Z), the 5&#x2032; side region (Xc), and the 3&#x2032; side region (Yc) includes the expression inhibitory sequence.

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Kurume, Japan

Tomohiro Hamasaki