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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
1998-4-9
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pubmed:abstractText |
We have determined that hexadeoxyribonucleotides (5'TGGGAG3'), with modified aromatic groups such as a trityl group at the 5'-end, have anti-HIV-1 activity in vitro. The 6-mer bearing a 3,4-dibenzyloxybenzyl (3,4-DBB) group at the 5'-end had the most potent activity and the least cytotoxicity. When the 3'-end of the 5'-(3,4-DBB)-modified 6-mer was substituted with a 2-hydroxyethylphosphate, a 2-hydroxyethylthiophosphate, or a methylphosphate group at the 3'-end, anti-HIV-1 activity increased. Moreover, among various 3'- and 5'-end-modified 6-mers that were tested, the 6-mer (R-95288) bearing a 3,4-DBB group at the 5'-end and a 2-hydroxyethylphosphate group at the 3'-end was the most stable, when incubated with mouse, rat, or human plasma. Therefore, R-95288 was chosen as the best candidate for possible use in therapy on the basis of its anti-HIV-1 activity.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0968-0896
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pubmed:author |
pubmed-author:AbeKK,
pubmed-author:AgatsumaTT,
pubmed-author:FurukawaHH,
pubmed-author:HotodaHH,
pubmed-author:KanekoMM,
pubmed-author:KimuraSS,
pubmed-author:KogaRR,
pubmed-author:KoizumiMM,
pubmed-author:KosakaTT,
pubmed-author:MomotaKK,
pubmed-author:NishigakiTT,
pubmed-author:OhmineTT,
pubmed-author:ShimadaKK,
pubmed-author:SoniNN,
pubmed-author:TsutsumiSS
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pubmed:issnType |
Print
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pubmed:volume |
5
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2235-43
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:9459021-Animals,
pubmed-meshheading:9459021-Anti-HIV Agents,
pubmed-meshheading:9459021-Cell Line,
pubmed-meshheading:9459021-Circular Dichroism,
pubmed-meshheading:9459021-HIV-1,
pubmed-meshheading:9459021-Humans,
pubmed-meshheading:9459021-Mice,
pubmed-meshheading:9459021-Models, Chemical,
pubmed-meshheading:9459021-Nucleic Acid Conformation,
pubmed-meshheading:9459021-Oligodeoxyribonucleotides,
pubmed-meshheading:9459021-Rats
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pubmed:year |
1997
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pubmed:articleTitle |
Biologically active oligodeoxyribonucleotides--IX. Synthesis and anti-HIV-1 activity of hexadeoxyribonucleotides, TGGGAG, bearing 3'- and 5'-end-modification.
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pubmed:affiliation |
Exploratory Chemistry Research Laboratory, Sankyo Co., Ltd., Tokyo, Japan. koizum@shina.sankyo.co.jp
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pubmed:publicationType |
Journal Article
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