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An unusual "senseless" 2',5'-oligoribonucleotide with potent anti-HIV activity
Tarek Aboul-Fadl1, Vijai K Agrawal, Robert W Buckheit
1Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, USA.
Abstract:
A new 32-mer 2',5'-oligoribonucleotide of 1-methyl-6-thioinosinic acid (10) has been synthesized. The design of this unique oligoribonucleotide is based on the reported HIV inhibitory activities of both 2',5'-oligonucleotides and the 3',5'-oligoribonucleotides containing the 1-methyl-6-mercaptopurine base. Tm and CD studies of 10 revealed that it has no organized secondary structure, presumably due to the rigidity of the molecule. The synthesized oligomer, 10, showed a potent inhibitory effect on HIV-1RF and significantly inhibited HIV-1 reverse transcriptase.
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