Napajen Pharma, Inc.

Napa Jenomics Co., Ltd.

Atsushi Uno

Kazuo Sakurai

Hideki Ohba

Hironori Ando

Takanori Kubo

Sadaharu Higuchi

Jusaku Minari

An objective of the present invention is to provide a chemically-modified siRNA that has polydeoxyadenylic acid added to the 5' end of the sense strand, and, when complexed with schizophyllan, is high in resistance against RNase and moreover effectively exhibits RNAi activity. To achieve the objective, in the chemically-modified siRNA with polydeoxyadenylic acid added to the 5&#x2032; end of the sense strand, specific chemical modification is performed for dinucleotide sequences of CA, UA, and UG in the base sequence of the sense strand and dinucleotide sequences of CA, UA, and UG in the base sequence at and after the eighth base from the 5&#x2032; end of the antisense strand.

Chemically-modified siRNA

An object of the present invention is to provide novel double-stranded RNA having an RNA interference effect, in which the cellular uptake and the resistance to enzymatic degradation are improved, without reducing the RNA interference effect. The cellular uptake and the resistance to enzymatic degradation of a complex of a polysaccharide having a &#x3b2;-1,3-glucan skeleton and double-stranded RNA can be significantly improved while maintaining the RNA interference effect, by fulfilling the following conditions (i) to (iii): (i) the double-stranded RNA has a sense strand consisting of a base sequence complementary to a target sequence in a target gene and an antisense strand containing a base sequence complementary to the sense strand, and the double-stranded RNA can inhibit expression of the target gene; (ii) the double-stranded RNA has a single-stranded polydeoxyadenine bound directly or via a linker to the end of at least one of the sense strand and the antisense strand; and (iii) the polysaccharide and the single-stranded polydeoxyadenine form a complex.

Complex of polysaccharide and double-stranded RNA

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Koganei, Japan

Atsushi Uno