Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

FTC Racemate [[[(2S,5R)-5-(4-amino-5- fluoro-2-oxo...

Synonyms: CHEMBL192771, CHEBI:423432, AC1LA5DO, (+)-FTC-TP, (+)-FTCTP, ...

Feng, J.Y. et al., Gao, H.Q. et al., Darque, A. et al.

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Disease relevance of AIDS-059447

Both of the mutations, M184I and M184V, provide very high levels of resistance in vivo; purified HIV-1 RT carrying M184V and M184I also shows resistance to 3TCTP and FTCTP in in vitro polymerase assays [1].
However, a detailed study of the incorporation of (-)FTC-TP by human mitochondrial DNA polymerase gamma, a host enzyme associated with nucleoside toxicity, is required for complete understanding of the molecular mechanisms of inhibition and toxicity [2].

Analytical, diagnostic and therapeutic context of AIDS-059447

The FTC-TP was subsequently digested to release the parent nucleoside that was finally analyzed by HPLC with UV detection (HPLC-UV) [3].

References

The role of steric hindrance in 3TC resistance of human immunodeficiency virus type-1 reverse transcriptase. Gao, H.Q., Boyer, P.L., Sarafianos, S.G., Arnold, E., Hughes, S.H. J. Mol. Biol. (2000) [Pubmed]
Relationship between antiviral activity and host toxicity: comparison of the incorporation efficiencies of 2',3'-dideoxy-5-fluoro-3'-thiacytidine-triphosphate analogs by human immunodeficiency virus type 1 reverse transcriptase and human mitochondrial DNA polymerase. Feng, J.Y., Murakami, E., Zorca, S.M., Johnson, A.A., Johnson, K.A., Schinazi, R.F., Furman, P.A., Anderson, K.S. Antimicrob. Agents Chemother. (2004) [Pubmed]
Quantitation of intracellular triphosphate of emtricitabine in peripheral blood mononuclear cells from human immunodeficiency virus-infected patients. Darque, A., Valette, G., Rousseau, F., Wang, L.H., Sommadossi, J.P., Zhou, X.J. Antimicrob. Agents Chemother. (1999) [Pubmed]

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