Some 6-aza-5-substituted-2'-deoxyuridines show potent and selective inhibition of herpes simplex virus type 1 thymidine kinase. (Articolo in rivista)

Type
Label
  • Some 6-aza-5-substituted-2'-deoxyuridines show potent and selective inhibition of herpes simplex virus type 1 thymidine kinase. (Articolo in rivista) (literal)
Anno
  • 1998-01-01T00:00:00+01:00 (literal)
Alternative label
  • Basnak I, Sun M, Hamor TA, Focher F, Verri A, Spadari S, Wroblowski B, Herdewijn P, Walker RT. (1998)
    Some 6-aza-5-substituted-2'-deoxyuridines show potent and selective inhibition of herpes simplex virus type 1 thymidine kinase.
    in Nucleosides & nucleotides
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Basnak I, Sun M, Hamor TA, Focher F, Verri A, Spadari S, Wroblowski B, Herdewijn P, Walker RT. (literal)
Pagina inizio
  • 187 (literal)
Pagina fine
  • 206 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 17 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Istituto di Genetica Molecolare, Pavia (literal)
Titolo
  • Some 6-aza-5-substituted-2'-deoxyuridines show potent and selective inhibition of herpes simplex virus type 1 thymidine kinase. (literal)
Abstract
  • The synthesis and X-ray crystal structures of a series of 5-substituted-6-aza-2'-deoxyuridines is reported. These nucleoside analogues inhibit the phosphorylation of thymidine by HSV-1 TK but have no effect on the corresponding human enzyme. Detailed examination of one analogue proves it to be a competitive inhibitor of thymidine with a Ki of 0.34 microM and is a very poor substrate. The analogues are not substrates for the enzyme and also do not inhibit the degradation of thymidine by thymidine phosphorylase. Molecular modelling showed that the inhibitors fit well in the active site of HSV-1 TK, provided the conformation of the sugar moiety is the same for thymidine in the complex. (literal)
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