Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2'-, 3'-, 5'-, nucleobase and internucleotide linkage sites. The folate can be attached via the α- or γ-carboxylate, optionally through a linking group. Methods for
Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2'-, 3'-, 5'-, nucleobase and internucleotide linkage sites. The folate can be attached via the α- or γ-carboxylate, optionally through a linking group. Methods for the regiospecific synthesis of the conjugates are disclosed.
대표청구항▼
Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2'-, 3'-, 5'-, nucleobase and internucleotide linkage sites. The folate can be attached via the α- or γ-carboxylate, optionally through a linking group. Methods for
Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2'-, 3'-, 5'-, nucleobase and internucleotide linkage sites. The folate can be attached via the α- or γ-carboxylate, optionally through a linking group. Methods for the regiospecific synthesis of the conjugates are disclosed. Protease", The Journal of Immunology, vol.145 No. 5, pp. 1469-1476, (1990). Shephard et al., "Characterization of neutrophil-mediated degradation of human C-reactive protein and identification of the protease", Clin. Exp. Immunol., vol. 87, pp.509-513, (1992). Shephard et al., "C-reactive protein (CRP) peptides inactive enolase in human neutrophil leading to depletion of intracellular ATP and inhibition of superposed generation", Immunology, vol.76, pp. 79-85, (1992). Yavin et al., "Proteolysis of human C-reactive protein by neutrophil-derived lysosomal enzymes generated peptides which modulate neutrophil function: Implication to the anti-inflammatory mechanism", Letters in Peptide Science, vol.2, pp.7-16, (1995). Yavin et al., "Synthetic peptides derived from the sequence of human C-reactive protein inhibit the enzymatic activities of human leukocyte elastase and human leukocyte cathepsin G", Int. J. Peptide Protein Res.,, vol.48, pp.465-476, (1996). Yavin et al., "Binding Pockets on the surface of human Leukocyte elastase and human leukocyte cathepsin G. Implications to the design of inhibitors derived from human C-reactive protein", Biomedical Peptides, Proteins & Nucleic Acids, vol.2, pp. 71-78, (1997). Yavin et al., "Inhibition of Human leukocyte elastase and cathepsin G by extending peptides and subunits derived from human C-reactive protein", Letters in Peptide Science, vol.4, pp. 157-166, (1997). Yavin et al., "Peptides Derived from Human C-reactive Protein Inhibit the Enzymatic Activities of Human Leukocyte Elastase and Cathespin G: use of Overlapping Peptide Sequences to Identify a Unique Inhibitor," Journal of Peptide Research, vol. 51, No. 4, Apr. 1998; pp. 282-289. Yavin et al., "Synthetic Peptides Derived from the Sequence of Human C-reactive Protein Inhibit the Enzymatic Activities of Human Leukocyte Elastase and Human Leukocyte Cathespin G," Inter. Journal of Peptide and Protein Research, vol. 48, No. 5, Nov. 1996, pp. 465-476. Yavin, E.A., "Binding Pockets on the Surface of Human Leukocyte Elastase and Human Leukocyte Cathespin G. Implications to the Design of Inhibitors Derived from Human C-Reactive Protein," Biomed. Peptides, Proteins & Nucleic Acids, vol. 2, 1997, pp. 71-78. Yavin, E.A. "Inhibition of the HLE and Cathespin G by Extended Peptides and Subunits Derived from Human C-reactive Protein," Letters in Peptide Science, vol. 4, No. 3, 1997, pp. 157-166. WO96/036286, WO; WO96/040281, WO; WO96/040285, WO; WO98/000172, WO; WO98/004292, WO; WO98/018501, WO; WO99/013919, WO; WO99/039738, WO; WO 00/45856, WO; WO 01/15742, WO
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Collard, Joseph; Khorkova Sherman, Olga, Treatment of tumor necrosis factor receptor 2 (TNFR2) related diseases by inhibition of natural antisense transcript to TNFR2.
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Collard, Joseph; Khorkova Sherman, Olga, Treatment of uncoupling protein 2 (UCP2) related diseases by inhibition of natural antisense transcript to UCP2.
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