One-third-the-sites transition-state inhibitors for purine nucleoside phosphorylase.

@article{Miles1998OnethirdthesitesTI,
  title={One-third-the-sites transition-state inhibitors for purine nucleoside phosphorylase.},
  author={Ronald W. Miles and Peter C Tyler and Richard H. Furneaux and Carey K. Bagdassarian and Vern L Schramm},
  journal={Biochemistry},
  year={1998},
  volume={37 24},
  pages={8615-21}
}
Genetic defects in human purine nucleoside phosphorylase cause T-cell deficiency as the major phenotype. It has been proposed that efficient inhibitors of the enzyme might intervene in disorders of T-cell function. Compounds with features of the transition-state structure of purine nucleoside phosphorylase were synthesized and tested as inhibitors. The transition-state structure for purine nucleoside phosphorylase is characterized by (1) an elevated pKa at N7 of the purine ring for protonation… CONTINUE READING

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