De Clercq E, Balzarini J, Bernaerts R, Herdewijn P, Verbruggen A
Biochem Biophys Res Commun. 1985 Jan 16;126(1):397-403. doi: 10.1016/0006-291x(85)90619-9.
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.
（E）-5-（2-溴乙烯基）-2'-脱氧尿苷（C-BVDU）和（E）-5-（2-碘乙烯基）-2'-脱氧尿苷（C-IVDU）的碳环类似物，其中糖部分被环戊烷环取代，与它们的母体化合物（BVDU和IVDU）一样，是单纯疱疹病毒1型（HSV-1）编码的胸苷激酶（TK）的有效底物。这一结论基于BVDU、IVDU、C-BVDU和C-IVDU对HSV-1 TK的结合亲和力（Ki）以及该酶对（125I）IVDU和（125I）C-IVDU的磷酸化速率（Km，Vmax）。病毒TK对C-BVDU和C-IVDU的特异性磷酸化可能解释了为什么这些化合物是HSV-1复制的高度选择性抑制剂。
