The enzymatic basis of cyclophosphamide specificity.

  title={The enzymatic basis of cyclophosphamide specificity.},
  author={H. J. Hohorst and Ludmilla Bielicki and Georg Voelcker},
  journal={Advances in enzyme regulation},
Metabolic activation of cyclophosphamide (CP) by microsomal mixed function hydroxylases yields 4-hydroxycyclophosphamide and aldophosphamide defined as activated CP. Activated CP shows relatively high cancerotoxic selectivity in vivo and cytotoxic specificity in vitro and can be trapped rapidly by reversible reaction of hemiaminal group of the oxazaphosphorine ring with protein thiols to form protein bound activated CP (protein-S-CP). Protein-S-CP stores activated CP in a highly stable form… CONTINUE READING