Oligonucleotides including pyrazolo[3,4-D]pyrimidine bases, bound in double stranded nucleic acids
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United States of America Patent
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Nov 7, 2000
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N/A
app pub date -
Apr 30, 1997
filing date -
Apr 30, 1997
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Expired
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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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