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Molecular Pharmacology, Vol 4, 402-404, Copyright © 1968 by the American Society for Pharmacology and Experimental Therapeutics

Some Observations on the Phosphorylation of Cytosine Arabinoside

DAVID KESSEL 1

1 Laboratories of Pharmacology, Children’s Cancer Research Foundation, and Department of Pathology, Harvard Medical School, Boston, Massachusetts 02115

Phosphorylation of cytosine arabinoside, a requisite for drug action, was catalyzed by deoxycytidine kinase. This reaction was strongly inhibited by deoxycytidine and by deoxycytidine nucleotides. An examination of kinetic data indicates the Ki for deoxycytidine was 40-fold smaller than the Km for cytosine arabinoside. This difference apparently explains one site of the reversal of cytosine arabinoside toxicity by deoxycytidine.

Note:
This work was supported, in part, by contract PH 43-66-541 from the Cancer Chemotherapy National Service Center, National Cancer Institute, National Institutes of Health. The author wishes to express his appreciation to Miss Marjorie Myers for assistance in this study.

Submitted on April 5, 1968






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