An unusual "senseless" 2′,5′-oligoribonucleotide with potent anti-HIV activity

被引:10
作者
Aboul-Fadl, T [1 ]
Agrawal, VK [1 ]
Buckheit, RW [1 ]
Broom, AD [1 ]
机构
[1] Univ Utah, Dept Med Chem, Salt Lake City, UT 84112 USA
关键词
oligoribonucleotide; HIV-1; reverse transcriptase; ssRNA;
D O I
10.1081/NCN-120030713
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 [生物化学与分子生物学]; 081704 [应用化学];
摘要
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-1(RF) and significantly inhibited HIV-1 reverse transcriptase.
引用
收藏
页码:545 / 554
页数:10
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