Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase
نویسندگان
چکیده
منابع مشابه
An interlocked dimeric parallel-stranded DNA quadruplex: a potent inhibitor of HIV-1 integrase.
We report on the NMR-based solution structure of the 93del d(GGGGTGGGAGGAGGGT) aptamer, a potent nanomolar inhibitor of HIV-1 integrase. This guanine-rich DNA sequence adopts an unusually stable dimeric quadruplex architecture in K+ solution. Within each 16-nt monomer subunit, which contains one A.(G.G.G.G) pentad sandwiched between two G.G.G.G tetrads, all G-stretches are parallel, and all gua...
متن کاملProgress in HIV-1 integrase inhibitors: A review of their chemical structure diversity
HIV-1 integrase (IN) enzyme, one of the three main enzymes of HIV-1, catalyzed the insertion of the viral DNA into the genome of host cells. Because of the lack of its homologue in human cells and its essential role in HIV-1 replication, IN inhibition represents an attractive therapeutic target for HIV-1 treatment. Since identification of IN as a promising therapeutic target, a major progress h...
متن کاملProgress in HIV-1 integrase inhibitors: A review of their chemical structure diversity
HIV-1 integrase (IN) enzyme, one of the three main enzymes of HIV-1, catalyzed the insertion of the viral DNA into the genome of host cells. Because of the lack of its homologue in human cells and its essential role in HIV-1 replication, IN inhibition represents an attractive therapeutic target for HIV-1 treatment. Since identification of IN as a promising therapeutic target, a major progress h...
متن کاملprogress in hiv-1 integrase inhibitors: a review of their chemical structure diversity
hiv-1 integrase (in) enzyme, one of the three main enzymes of hiv-1, catalyzed the insertion of the viral dna into the genome of host cells. because of the lack of its homologue in human cells and its essential role in hiv-1 replication, in inhibition represents an attractive therapeutic target for hiv-1 treatment. since identification of in as a promising therapeutic target, a major progress h...
متن کاملA triple helix-forming oligonucleotide-intercalator conjugate acts as a transcriptional repressor via inhibition of NF kappa B binding to interleukin-2 receptor alpha-regulatory sequence.
Oligonucleotide-directed triplex formation within upstream regulatory sequences is envisioned as a potential tool for gene inhibition. However, this approach requires that triple helix-forming oligonucleotides are chemically modified, so that the triplex is stable under physiological conditions. Here, we have compared several chemical modifications of an oligonucleotide, targeted to a natural 1...
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ژورنال
عنوان ژورنال: FEBS Letters
سال: 1999
ISSN: 0014-5793
DOI: 10.1016/s0014-5793(99)01350-2