Insight into the Mechanism of the Stabilization of Moloney Murine Leukaemia Virus Reverse Transcriptase by Eliminating RNase H Activity

2010 ◽  
Vol 74 (2) ◽  
pp. 440-442 ◽  
Author(s):  
Masaki MIZUNO ◽  
Kiyoshi YASUKAWA ◽  
Kuniyo INOUYE
Keyword(s):  
Reverse Transcriptase ◽  
Rnase H ◽  
Leukaemia Virus ◽  
Murine Leukaemia Virus ◽  
Insight Into ◽  
Moloney Murine Leukaemia Virus

scholarly journals Inhibition of murine leukaemia virus reverse transcriptase by 2-halogenated polyadenylic acids

1982 ◽  
Vol 203 (3) ◽  
pp. 755-760 ◽  
Author(s):  
T Fukui ◽  
E De Clercq
Keyword(s):  
Reverse Transcriptase ◽  
Dna Polymerase ◽  
Reverse Transcriptase Activity ◽  
Leukaemia Virus ◽  
Transcriptase Activity ◽  
Murine Leukaemia Virus ◽  
Polyadenylic Acid ◽  
Moloney Murine Leukaemia Virus

Several new analogues of polyadenylic acid [(A)n], i.e. poly(2-fluoroadenylic acid) [(fl2A)n], poly(2-chloroadenylic acid [(cl2A)n], poly(2-bromoadenylic acid) [(br2A)n] and poly(2-iodoadenylic acid) [(io2A)n] have been synthesized and evaluated for their effects on the RNA-directed DNA polymerase (reverse transcriptase) activity of Moloney murine leukaemia virus. All (A)n analogues were found to be potent inhibitors of reverse transcriptase, the order of (decreasing) potency being (fl2A)n greater than (io2A)n greater than (br2A)n greater than (cl2A)n. For all four (A)n analogues the inhibition of reverse transcriptase was competitive with respect to the template-primer. (A)n . oligo(dT). The K1 values were 0.02 microgram/ml for (fl2A)n, 0.1 microgram/ml for (io2A)n, 0.5 microgram/ml for (br2A)n and 8 microgram/ml for (cl2A)n. With a Ki of 0.02 microgram/ml (approx. 0.04 microM), (fl2A)n can be considered as one of the most, if not the most, potent polynucleotide inhibitor of reverse transcriptase that has been described so far.

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