Modified oligonucleotides

Details Modified oligonucleotides Modified oligonucleotides

1988-11-14

1992-05-12

Wax, Robert A.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 28, 536 29, 435 6, C12Q 168, C07H 1512

Patent

active

051129639

ABSTRACT:
The present invention provides modified oligonucleotides, wherein, amongst the first four bases on the 5'-end, they have the base sequence AT or TA and, bound to one of the two O.sup.- groups of the 5'-phosphate group of the first nucleotide at the 5'-end of said oligonucleotide, they contain a radical of the general formula: ##STR1## in which R.sub.4 is a spacer group and R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms or alkyl or alkoxy radicals containing up to 3 carbon atoms.
These modified oligonucleotides can be used for blocking the replication and/or expression of genes which have a sequence complementary with the modified oligonucleotides.

REFERENCES:
patent: 4196281 (1980-04-01), Hearst
patent: 4835263 (1989-05-01), Nguyen et al.
Miller, Paul S. Jerusalem Symp. Quantum Chem. Biochem. 1985, "Control of e expression by oligonucleotide methylphosphonate" pp. 207-219, abstr. in CA 104:220115x, 1985.
Isaacs, et al. (1982) "Trends in Photobiology" ed. C. Helene et al. Plenum Press, New York, pp. 279-294.
Bachellerie, J. P. et al. (1981) Nucl. Acids Res. 9:2207-2222.
Cazenave et al. (1989) Nucleic Acid Res. 17:4255-4271.
Louis J. Maher III and Bruce J. Dolnick (1988) Nuc. Acid Res. 16:3341-3358.

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