A novel metabolic effect of the adenosine deaminase inhibitor coformycin (cas 11033-22-0), a potentiator of antiviral adenosine analogues

Add time:08/17/2019    Source:sciencedirect.com

Coformycin [(R)-3-(β-d-erythropentofuranosyl)-3,6,7,8-tetrahydroimidazo [4,5 d]-[1,3] diazepin-8-(R)-ol] is an inhibitor of adenosine deaminase and thus increases the antiviral potency of a series of adenosine analogues. The influence of chemically synthesized coformycin triphosphate on RNA-polymerizing enzymes (RNA polymerases from E. coli and from calf thymus, poly(A) polymerase) and on DNA-synthesizing enzymes (DNA polymerases and terminal deoxynucleotidyltransferase from calf thymus) was studied. Only the poly(A) polymerase was found to be sensitively inhibited by coformycin triphosphate. The inhibition is non-competitive with respect to ATP (Ki = 2.9 μM). Inhibition was reversed by simple dilution. The inhibitor does not act as chain terminator.

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