Inhibition of avian myeloblastosis virus reverse transcriptase by diphosphates of acyclic phosphonylmethyl nucleotide analogues
Jazyk angličtina Země Nizozemsko Médium print
Typ dokumentu časopisecké články
PubMed
1699492
DOI
10.1016/0166-3542(90)90013-w
PII: 0166-3542(90)90013-W
Knihovny.cz E-zdroje
- MeSH
- adenin analogy a deriváty MeSH
- antivirové látky farmakologie MeSH
- cytosin analogy a deriváty MeSH
- fosfáty farmakologie MeSH
- guanin analogy a deriváty MeSH
- inhibitory reverzní transkriptasy * MeSH
- kur domácí MeSH
- nukleotidy farmakologie MeSH
- thymidin analogy a deriváty MeSH
- uracil analogy a deriváty MeSH
- virus ptačí myeloblastózy účinky léků enzymologie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- adenin MeSH
- antivirové látky MeSH
- cytosin MeSH
- fosfáty MeSH
- guanin MeSH
- inhibitory reverzní transkriptasy * MeSH
- nukleotidy MeSH
- thymidin MeSH
- uracil MeSH
Diphosphates of N-(2-phosphonylmethoxyethyl) derivatives of heterocyclic bases were studied in the endogenous oligo(dT)12-18 primed reaction of reverse transcriptase from detergent-disrupted AMV(MAV) retrovirions. These diphosphates (analogues of nucleotide 5'-triphosphates) exhibited an inhibitory activity towards reverse transcriptase. This inhibitory activity was dependent on the character of the heterocyclic base and decreased in the order: 2-aminoadenine greater than adenine greater than guanine much greater than cytosine much greater than thymine greater than uracil. The 2-aminoadenine derivative was more potent than either AZT-TP or ddTTP, while PMEApp had approximately the same potency as the two reference compounds (IC50 approximately 1 microM at 20 microM competing substrate). This finding is consistent with the antiviral activity of the parent nucleotide analogues against retroviruses (including HIV).
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