The effect of certain N-tritylated phenylalanine conjugates of amino-adenosine-3',5'-cyclic monophosphate on moloney murine leukaemia virus reverse transcriptase activity

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dc.contributor.authorVan Zyl, Johann M.
dc.contributor.authorAriatti, Mario
dc.contributor.authorHawtrey, Arthur O.
dc.date.accessioned2011-05-15T15:55:09Z
dc.date.available2011-05-15T15:55:09Z
dc.date.issued2010-07
dc.descriptionThe original publication is available at http://www.sajs.co.za/en_ZA
dc.description.abstractMoloney murine leukaemia virus M-MuLV) is a member of the retrovirus family. Its cloned reverse transcriptase RT), similarly to HIV type 1 reverse transcriptase HIV-1 RT), exhibits DNA-polymerase and ribonuclease H RNase H) activities capable of converting the single-stranded retroviral RNA genome into double-stranded DNA. The latter is then integrated into the host chromosome during viral infection. M-MuLV RT is, therefore, an attractive enzyme to help understand mutations in HIV-1 RT and its use in inhibition studies can help facilitate new drug designs. In this study, conjugates consisting of N-trityl derivatives of p-fluoro, p-nitro and p-iodo-DL-phenylalanine were coupled to 8-6-aminohexyl) amino-adenosine-3',5'-cyclic monophosphate and examined for their effect on DNA synthesis by M-MuLV RT. Synthesis was studied in a system containing poly rA).oligo dpT)15 as a template-primer with [ 3H] dTTP. The iodo-derivative, N-trityl-p-iodo-DL-phenylalanine-8-6- aminohexyl) amino-adenosine-3',5'-cyclic monophosphate was found to be a very active inhibitor of the RT enzyme IC50 = 1 μM), while the p-nitro IC50 = 45 μM) and p-fluoro IC50 = 65 μM) were weak inhibitors. Further work will be aimed at determining the mode of binding of the N-tritylated conjugates and also of various substituted amino acids and short peptides to M-MuLV RT to elucidate the mechanisms of inhibition. © 2010. The Authors.en_ZA
dc.description.versionPublishers' version
dc.format.extent5 p. : ill.
dc.identifier.citationVan Zyl, J. M., Ariatti, M. & Hawtrey, A. O. 2010. The effect of certain N-tritylated phenylalanine conjugates of amino-adenosine-3',5'-cyclic monophosphate on moloney murine leukaemia virus reverse transcriptase activity. South African Journal of Science, 106(7/8), doi:10.4102/sajs.v106i7/8.195.en_ZA
dc.identifier.issn1996-7489 (online)
dc.identifier.issn0038-2353 (print)
dc.identifier.otherdoi:10.4102/sajs.v106i7/8.195
dc.identifier.urihttp://hdl.handle.net/10019.1/9613
dc.language.isoen_ZA
dc.publisherAcademy of Science of South Africa (ASSAf)en_ZA
dc.rights.holderAuthors retain copyrighten_ZA
dc.subjectLeukemiaen_ZA
dc.subjectMoloney murine leukaemia virusen_ZA
dc.titleThe effect of certain N-tritylated phenylalanine conjugates of amino-adenosine-3',5'-cyclic monophosphate on moloney murine leukaemia virus reverse transcriptase activityen_ZA
dc.typeArticleen_ZA
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