Ono K, Nakane H, Colla L, De Clercq E
Nucleic Acids Symp Ser. 1983(12):123-6.
(E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate (BVdUTP), known as a specific inhibitor of herpes simplex virus (type 1)-DNA polymerase, was found to be a potent inhibitor of the activity of terminal deoxynucleotidyltransferase (TdT) from calf thymus. BVdUTP was not an efficient substrate of TdT, but it inhibited the incorporation of normal deoxynucleotide substrates in competitive fashion at the nucleotide binding site of TdT molecule. The Ki value for BVdUTP (5 microM) was much less than the Km value for dGTP (83 microM), indicating stronger affinity of the inhibitor to TdT than that of the substrate. These results indicate the usefulness of BVdUTP as a potent inhibitor of TdT for elucidation of the reaction mechanism of this enzyme.
（E）-5-（2-溴乙烯基）-2'-脱氧尿苷5'-三磷酸（BVdUTP），作为单纯疱疹病毒（1型）-DNA聚合酶的特异性抑制剂，被发现是小牛胸腺末端脱氧核苷酸转移酶（TdT）活性的有效抑制剂。BVdUTP不是TdT的有效底物，但它在TdT分子的核苷酸结合位点以竞争方式抑制正常脱氧核苷酸底物的掺入。BVdUTP的Ki值（5 microM）远小于dGTP的Km值（83 microM），表明该抑制剂对TdT的亲和力强于底物。这些结果表明BVdUTP作为TdT的有效抑制剂对于阐明该酶的反应机制是有用的。
