METABOLISM OF GS-7340, A NOVEL PHENYL MONOPHOSPHORAMIDATE INTRACELLULAR PRODRUG OF PMPA, IN BLOOD

@article{Eisenberg2001METABOLISMOG,
  title={METABOLISM OF GS-7340, A NOVEL PHENYL MONOPHOSPHORAMIDATE INTRACELLULAR PRODRUG OF PMPA, IN BLOOD},
  author={Eugene J. Eisenberg and Gong Xin He and William A. Lee},
  journal={Nucleosides, Nucleotides \& Nucleic Acids},
  year={2001},
  volume={20},
  pages={1091 - 1098}
}
PMPA, an acyclic nucleoside phosphonate analog, is a potent inhibitor of HIV. In the cells, PMPA is efficiently phosphorylated by intracellular kinases to produce PMPApp, the pharmacologically active metabolite. Despite its demonstrated antiviral potency, PMPA has limited cell permeability presumably resulting from the presence of two negative charges on the phosphonyl group. To enhance intracellular concentrations of PMPA, we developed a prodrug, selectively metabolized inside cells. GS-7340… 
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