Nucleotide analogue inhibitors of purine nucleoside phosphorylase.

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Nucleotide analogue inhibitors of purine nucleoside phosphorylase.

The diphosphate of the antiherpetic agent acyclovir [9-[(2-hydroxyethoxy)methyl]guanine] has been shown to inhibit purine nucleoside phosphorylase with unique potency (Tuttle, J. V., and Krenitsky, T. A. (1984) J. Biol. Chem. 259, 4065-4069). A major factor contributing to the superior inhibition by this diphosphate over the corresponding mono- and triphosphates is revealed here. Homologues of ...

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Murine purine nucleoside phosphorylase (PNP) has been cloned and sequenced. An ICR macrophage murine cDNA library (Clontech Laboratories) was screened with a 246 base pair (bp) RNA probe to the 3' coding region of human PNP (1) (obtained from S.R.Williams). Seven clones were obtained, their sequence spanning 1161 bp. The deduced amino acid (AA) sequence of an open reading frame from bp 3 to 770...

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Achieving the ultimate physiological goal in transition state analogue inhibitors for purine nucleoside phosphorylase.

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1. Concave-downward double-reciprocal plots were obtained for rabbit erythrocyte purine nucleoside phosphorylase when the concentration of Pi was varied over a wide range at a fixed saturating concentration of either inosine or deoxyinosine. Similar behaviour was also displayed by the calf spleen enzyme. 2. The degree of curvature of double-reciprocal plots was greatly modified by the presence ...

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ژورنال

عنوان ژورنال: Journal of Biological Chemistry

سال: 1990

ISSN: 0021-9258

DOI: 10.1016/s0021-9258(19)39734-0