PT  - JOURNAL ARTICLE
AU  - Y.-C. CHENG
AU  - G. DUTSCHMAN
AU  - E. DE CLERCQ
AU  - A. S. JONES
AU  - S. G. RAHIM
AU  - G. VERHELST
AU  - R. T. WALKER
TI  - Differential Affinities of 5-(2-Halogenovinyl)-2'-Deoxyuridines for Deoxythymidine Kinases of Various Origins
DP  - 1981 Jul 01
TA  - Molecular Pharmacology
PG  - 230--233
VI  - 20
IP  - 1
4099  - http://molpharm.aspetjournals.org/content/20/1/230.short
4100  - http://molpharm.aspetjournals.org/content/20/1/230.full
SO  - Mol Pharmacol1981 Jul 01; 20
AB  - The inhibition constants (Ki) of a series of 5-(2-halogenovinyl)-2'-deoxyuridines, including E-5-(2-chlorovinyl)-dUrd, E-5-(2-bromovinyl)-dUrd, E-5-(2-iodovinyl)-dUrd, and Z-5-(2-bromovinyl)-dUrd, have been determined for the dThd kinases of human cytosol or mitochondria, herpes simplex virus type 1 (HSV-1) or type 2 (HSV-2), or varicella-zoster virus (VZV). The E-5-(2-halogenovinyl)-2'-deoxyuridines had a much higher affinity for HSV-1 (or VZV) dThd kinase than for HSV-2 dThd kinase, and the affinity of E-5-(2-bromovinyl)-dUrd for HSV-1 dThd kinase was also much higher than that of its stereo-isomer, Z-5-(2-bromovinyl)-dUrd. The relative affinities of these compounds for the virus-induced dThd kinase correlated closely with their inhibitory effects on these viruses, suggesting that the selectivity of E-5-(2-bromovinyl)-dUrd and its congeners toward herpes viruses (HSV and VZV) is to a large extent dependent on their phosphorylation by the virus-induced dThd kinase.