Synthesis and biological activity of a bivalent nucleotide inhibitor of ribonucleotide reductase

  • Bioorg Med Chem Lett. 2000 Oct 16;10(20):2387-9. doi: 10.1016/s0960-894x(00)00481-9.
X Wu  1 B S Cooperman
Affiliations
  • 1. Department of Chemistry, University of Pennsylvania, Philadelphia 19104-6323, USA.
Abstract

A novel nucleotide inhibitor (ADP-S-HBES-S-dGTP) of mouse ribonucleotide reductase was designed to span the active site and the allosteric specificity site of the enzyme. The inhibitor contains ADP and dGTP moieties which are linked by 1,6-hexane-(bis-ethylenesulfone), and has a Ki value of 12 microM.

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