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  Synthesis of 21,31,51-trideoxyuridine-51-methylphosphonic acid and its diphosphate derivative. Study of the interaction with HIV-1reverse transcriptase

Benzaria, S., Maury, G., Gosselin, G., Rittinger, K., Divita, G., Goody, R., et al. (1994). Synthesis of 21,31,51-trideoxyuridine-51-methylphosphonic acid and its diphosphate derivative. Study of the interaction with HIV-1reverse transcriptase. Antiviral Chemistry & Chemotherapy, 5(4), 221-228. doi:10.1177/095632029400500403.

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AntivirChemChemother_5_1994_221.pdf (Any fulltext), 517KB
 
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Benzaria, S., Author
Maury, G., Author
Gosselin, G., Author
Rittinger, Katrin1, Author              
Divita, Gilles1, Author              
Goody, R.S1, Author              
lmbach, J.-L., Author
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1Emeritus Group Biophysics, Max Planck Institute for Medical Research, Max Planck Society, ou_1497712              

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 Abstract: 2′,3′,5′-Trideoxyuridine-5′-methylphosphonate, [8], was synthesized from ddU. The 5′,6′ carbon-carbon bond was formed by condensing the 5′-aldehyde of ddU and a Wittig reagent. The binding interaction of the diphosphate derivative [10] of the phosphonate [8] with HIV-1 reverse transcriptase (RT) was studied using methods based primarily on fluorescence spectroscopy. From the quenching of intrinsic tryptophan fluorescence of RT during its titration against [10], a dissociation constant of 24 μm was calculated at 25°C. In the presence of a DNA/DNA template/primer of defined sequence and RT, [10] and a fluorescent derivative of ddTTP competed for binding to RT without incorporation of ddU-5′-methylphosphonate. In the presence of a 0.5 mm concentration of [10], the RT activity measured with Poly(rA)/(dT)15 and [3H] dTTP was lowered to 65%. All our observations are consistent with suppression of the catalysis of bond formation between the OH at the primer 3′-end and α-P of [10] after formation of the complex between RT, template/primer and [10].

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Language(s): eng - English
 Dates: 1993-11-221993-10-301993-12-201994-08-01
 Publication Status: Published in print
 Pages: 8
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1177/095632029400500403
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Title: Antiviral Chemistry & Chemotherapy
Source Genre: Journal
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Publ. Info: Oxford [u.a.] ; Berlin : Blackwell
Pages: - Volume / Issue: 5 (4) Sequence Number: - Start / End Page: 221 - 228 Identifier: ISSN: 0956-3202