Aoyama H
Departamento de Bioquimica, Universidade Estadual de Campinas, São Paulo, Brasil.
Mol Cell Biochem. 1991 Dec 11;108(2):169-74. doi: 10.1007/BF00233122.
Nalidixic acid, a very specific inhibitor of bacterial DNA synthesis, has been studied for its action on the avian myeloblastosis virus reverse transcriptase activity. The drug inhibited the DNA synthesis reaction catalyzed by the viral enzyme in the presence of different template-primers. The inhibitory effect by nalidixic acid was higher with polyriboadenylic acid than with polyribocytidylic acid as a synthetic template. With activated DNA as a template nalidixic acid preferentially inhibited the TMP incorporation when compared with the dAMP incorporation. Both these results showed the importance of the presence of adenine in the templates for a more efficient inhibition by nalidixic acid. The inhibition for this drug was also shown in the presence of Mn2+ instead of Mg2+ as the divalent cation, and with a 2'-fluorinated analogue of polyriboadenylic acid as the template. Kinetic data showed a non-competitive inhibition by nalidixic acid in relation to polyriboadenylic acid and to TTP in the reaction catalyzed by reverse transcriptase.
萘啶酸是一种非常特异的细菌DNA合成抑制剂，已对其作用于禽成髓细胞瘤病毒逆转录酶活性进行了研究。该药物在存在不同模板引物的情况下抑制了由病毒酶催化的DNA合成反应。以聚核糖腺苷酸作为合成模板时，萘啶酸的抑制作用比以聚核糖胞苷酸时更高。与以dAMP掺入相比，以活化DNA作为模板时，萘啶酸优先抑制TMP掺入。这两个结果均表明模板中腺嘌呤的存在对于萘啶酸更有效的抑制作用很重要。在以Mn2+而非Mg2+作为二价阳离子，以及以聚核糖腺苷酸 的2'-氟代类似物作为模板的情况下，也显示出该药物的抑制作用。动力学数据表明，在逆转录酶催化的反应中，萘啶酸对聚核糖腺苷酸和TTP呈非竞争性抑制。
