Oligonucleotides including pyrazolo[3,4-D]pyrimidine bases, boun

Details Oligonucleotides including pyrazolo[3,4-D]pyrimidine bases, boun Oligonucleotides including pyrazolo[3,4-D]pyrimidine bases, boun

1997-04-30

2000-11-07

Marschel, Ardin H.

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

Organic compounds

Carbohydrates or derivatives

435 6, 436501, 536 253, C07H 2100, C07H 2102, C07H 2104

Patent

active

061438774

ABSTRACT:
A triplex forming oligonucleotide is complementary pursuant to the G/T or A/G recognition motif to a homopurine, or substantially homopurine target sequence in double stranded nucleic acids, and at least one and preferably all of the guanine bases are replaced by their pyrazolo[3,4-d]pyrimidine analog, namely by 6-amino-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one. The oliginucleotides containing the pyrazolo[3,4-d]pyrimidine analog of guanine exhibit a lesser degree of self-association, and lack the nucleophilic nitrogen atom in the 7 position of guanine. The latter feature results in a diminished extent of self-crosslinking in ODNs which also have a covalently attached cross-linking agent.

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