Title: Selective antiherpetic activity of carbocyclic analogues of (E)-5-(2-halogenovinyl)-2'-deoxyuridines: dependence on specific phosphorylation by viral thymidine kinase
Authors: De Clercq, Erik ×
Balzarini, Jan
Bernaerts, R
Herdewijn, Piet
Verbruggen, Alfons #
Issue Date: 1985
Publisher: Academic press inc jnl-comp subscriptions
Series Title: Biochemical and Biophysical Research Communications vol:126 issue:1 pages:397-403
Abstract: The carbocyclic analogues of (E)-5-(2-bromovinyl)-2'-deoxyuridine (C-BVDU) and (E)-5-(2-iodovinyl)-2'-deoxyuridine (C-IVDU), in which the sugar moiety is replaced by a cyclopentane ring, are as efficient substrates for the herpes simplex type 1 (HSV-1)-encoded thymidine kinase (TK) as their parent compounds (BVDU and IVDU). This conclusion is based on the binding affinities (Ki) of BVDU, IVDU, C-BVDU and C-IVDU to the HSV-1 TK and on the phosphorylation rates (Km, Vmax) of (125I)IVDU and (125I)C-IVDU by the enzyme. The specific phosphorylation of C-BVDU and C-IVDU by the viral TK may explain why these compounds are highly selective inhibitors of HSV-1 replication.
ISSN: 0006-291X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Medicinal Chemistry (Rega Institute)
Radiopharmaceutical Research
× corresponding author
# (joint) last author

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