Enzymatic production of optically pure (2'R-cis)-2'-deoxy-3'-thiacytidine (3TC, lamivudine): a potent anti-HIV agent.

@article{Mahmoudian1993EnzymaticPO,
  title={Enzymatic production of optically pure (2'R-cis)-2'-deoxy-3'-thiacytidine (3TC, lamivudine): a potent anti-HIV agent.},
  author={Massoud Mahmoudian and B S Baines and Christopher s. Drake and Rowland Hale and Philip Edward Jones and J E Piercey and David S. Montgomery and Ian J. Purvis and Richard Storer and Michael J Dawson},
  journal={Enzyme and microbial technology},
  year={1993},
  volume={15 9},
  pages={749-55}
}
Although equipotent in terms of antiviral activity, the two enantiomers of 2'-deoxy-3'-thiacytidine (BCH 189) differ markedly in their cytotoxicity. (2'R-cis)-2'-deoxy-3'-thiacytidine (3TC) is substantially less toxic than its optical antipode, and is undergoing development for the therapy of HIV infection. Cytidine deaminase from Escherichia coli is shown here to deaminate 2'-deoxy-3'-thiacytidine enantioselectively to leave 3TC essentially optically pure. This reaction has been used to… CONTINUE READING

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