Li L H, Cowie C H, Gray L G, Moran D M, Clark T D, Rinehart K L
J Natl Cancer Inst. 1977 Feb;58(2):239-43. doi: 10.1093/jnci/58.2.239.
The activities of streptovaricin complexes, streptovaricins, streptovals, and streptovarinic degradation products were elevated against RNA-directed DNA polymerases of Rauscher leukemia virus, DNA-dependent DNA polymerase of bacterial and mammalian cells, and DNA-dependent RNA polymerases of mammalian origin. The activities of streptovaricins were also listed for comparison purposes. The effects of streptovaricin complexes on viral DNA polymerases varied significantly from lot to lot, and streptovaricin complex lot 7 was the most active. All the streptovals and streptovaricin degradation products except varicinal A showed a marked improvement (twofold to tenfold) in activity against the viral enzyme over the parent streptovaricins. None of these compounds, however, displayed any significant effect on either the DNA polymerase of L1210 leukemia cells and Escherichia coli or the RNA polymerase of isolated nuclei of mouse liver. As a result of tests in these systems, some specific inhibitors of RNA-directed DNA polymerases of Rauscher leukemia virus were selected.
链黑菌素复合物、链黑菌素、链黑菌素类似物及链黑菌素降解产物对劳斯氏白血病病毒的RNA指导的DNA聚合酶、细菌和哺乳动物细胞的DNA依赖性DNA聚合酶以及哺乳动物来源的DNA依赖性RNA聚合酶的活性均有所提高。为作比较,还列出了链黑菌素的活性。不同批次的链黑菌素复合物对病毒DNA聚合酶的作用差异显著,其中第7批链黑菌素复合物活性最强。除A变种外,所有链黑菌素类似物及链黑菌素降解产物对病毒酶的活性比母体链黑菌素均有显著提高(两倍至十倍)。然而,这些化合物对L1210白血病细胞和大肠杆菌的DNA聚合酶或小鼠肝脏分离细胞核的RNA聚合酶均无明显作用。通过这些系统的测试,筛选出了一些劳斯氏白血病病毒RNA指导的DNA聚合酶的特异性抑制剂。