Solstar Pharma has developed an siRNA platform technology using proprietary modified nucleic acid chemistry. Our modified nucleotides enhance the stability and optimize the mRNA target activity of our siRNAs.
We are harnessing the power of siRNA to inhibit pathogen replication such as in coronavirus disease or block the production of cancer-causing proteins.
Gene-based nucleic acid therapeutic technologies, such as RNA interference (RNAi), for sequence-specific target mRNA degradation, include small interfering RNA (siRNA). These oligonucleotide therapeutics are applied to direct mRNA degradation. We focus on siRNA-based therapeutics by applying our modified nucleotide platform technology.
siRNA enters the cell as a double stranded RNA molecule
One siRNA strand is recruited by the RISC complex
RISC + siRNA binds to a complementary mRNA
mRNA is cleaved in a specific site
Cleaved mRNA is degraded in the cell
Our siRNAs are designed using sequence algorithms and optimized to target specific disease-causing genes.
Solstar Pharma has developed novel nucleotides that contain modifications on the ribose sugar,
5′-C-aminopropyl-2′-O-methyl, which are applicable to siRNAs. These monomers significantly increase the stability of siRNAs by protecting them from nucleolytic degradation.
Structure of 5′-aminopropyl-nucleotides (5’ AA-Nt)
Nucleoside derivative and use therefor (4’-AminoAlchyl Nucleosides)
STATUS: JAPAN – Patent No. 7016170
Antiviral silencing RNA molecules, chemically modified antiviral silencing RNA molecules with enhanced cell penetrating abilities, pharmaceutical compositions comprising same and uses thereof for treatment of viral infections
STATUS: Published
Nucleoside derivative and use thereof (5’-AminoPropyl Nucleosides)
STATUS: JAPAN – Patent No. 7173467
Nucleoside derivative and use therefor (4’-AminoAlchoxyl Nucleosides)
STATUS: Published
Extended release gastroretentive formulation against helicobacter pylori
STATUS: Published
RNA interference agent, multiple chemically modified oligonucleotide, and use thereof
STATUS: Examination
Tsukimura, R., Kajino, R., Zhou, Y., Chandela, A., Ueno, Y.*: 4′-C-Aminoethoxy modification enhanced nuclease resistance of RNAs and improved thermal stability of RNA duplexes. Results in Chemistry 3: 100231, 2021.
Kajino, R. and Ueno, Y.*: (S)-5′-C-Aminopropyl-2′-O-methyl nucleosides enhance antisense activity in cultured cells and binding affinity to complementary single-stranded RNA. Bioorg. Med. Chem. 30: 115925, 2021.
Zhou, Y., Kajino, R., Ishii, S., Yamagishi, K. and Ueno, Y.*: Synthesis and evaluation of (S)-5′-C-aminopropyl and (S)-5′-C-aminopropyl-2′-arabinofluoro modified DNA oligomers for novel RNase H-dependent antisense oligonucleotides. RSC Advances 10: 41901-41914, 2020.
Tsuchihira, T., Kajino, R., Maeda, Y. and Ueno, Y.*: 4′-C-Aminomethyl-2′-deoxy-2′-fluoroarabinonucleoside increases the nuclease resistance of DNA without inhibiting the ability of a DNA/RNA duplex to activate RNase H. Bioorg. Med. Chem. 28: 115611, 2020.
Uematsu, A., Kajino, R., Maeda, Y. and Ueno, Y.*: Synthesis and characterization of 4′-C-guanidinomethyl-2′-O-methyl-modified RNA oligomers. Nucleotides & Nucleic Acids 39: 280-291, 2020.
Kajino, R., Maeda, Y., Yoshida, H., Yamagishi, K. and Ueno, Y.*: Synthesis and biophysical characterization of RNAs containing (R)- and (S)-5′-C-aminopropyl-2′-O-methyluridines. J. Org. Chem. 84: 3388-3404, 2019.
Kano, T., Katsuragi, Y., Maeda, Y. and Ueno, Y.*: Synthesis and properties of 4′-C-aminoalkyl-2′-fluoro-modified RNA oligomers. Bioorg. Med. Chem. 26: 4574-4582, 2018.
Koizumi, K., Maeda, Y., Kano, T., Yoshida, H., Sakamoto, T., Yamagishi, K. and Ueno, Y.*: Synthesis of 4′-C-aminoalkyl-2′-O-methyl modified RNA and their biological properties. Bioorg. Med. Chem. 26: 521-3534, 2018.
