An unusual "senseless" 2',5'-oligoribonucleotide with potent anti-HIV activity.
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.
Aboul-Fadl
Tarek
T
Department of Medicinal Chemistry, University of Utah, Salt Lake City, Utah 84112, USA.
Agrawal
Vijai K
VK
Buckheit
Robert W
RW
Broom
Arthur D
AD
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015497:HIV-1 / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D009843:Oligoribonucleotides / Q000737:chemistry* / Q000378:metabolism*; D017433:Protein Structure, Secondary; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013873:Thionucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
C488693:2',5'-oligo(1-methyl-6-thioinosinic acid); D019380:Anti-HIV Agents; D009843:Oligoribonucleotides; D018894:Reverse Transcriptase Inhibitors; D013873:Thionucleotides; D054303:HIV Reverse Transcriptase