De Clercq E
Cancer Lett. 1979 Nov;8(1):9-22. doi: 10.1016/0304-3835(79)90017-x.
Suramin--a well-known antitrypanosomal agent--was found to exert a strong inhibitory effect on the RNA-directed DNA polymerase (reverse transcriptase) activity of several oncornaviruses such as Moloney murine leukemia virus, murine Rauscher leukemia viruses, Moloney murine sarcoma virus and avian myeloblastosis virus. Inhibition of enzyme activity was obtained with both endogenous viral RNA and (A)n . oligo(dT) as the template-primer. Suramin effected a 50% inhibition of the reverse transcriptase activity of oncornaviruses at a concentration range of 0.1--1 microgram/ml. In this aspect it compared favorably to ethidium bromide, another trypanocide drug which is considered as one of the most powerful inhibitors of oncornaviral DNA polymerases. The inhibition of reverse transcriptase activity by suramin was competitive with the template-primer, (A)n . oligo(dT), suggesting that the drug may interact with the template-primer binding site of the enzyme.
苏拉明——一种著名的抗锥虫剂——被发现对几种肿瘤病毒如莫洛尼鼠白血病病毒、鼠劳舍尔白血病病毒、莫洛尼鼠肉瘤病毒和禽成髓细胞瘤病毒的RNA指导的DNA聚合酶(逆转录酶)活性具有强烈的抑制作用。以内源性病毒RNA和(A)n·寡聚(dT)作为模板引物均能抑制酶活性。苏拉明在0.1 - 1微克/毫升的浓度范围内能使肿瘤病毒的逆转录酶活性受到50%的抑制。在这方面,它与溴化乙锭相比具有优势,溴化乙锭是另一种杀锥虫药物,被认为是肿瘤病毒DNA聚合酶最有效的抑制剂之一。苏拉明对逆转录酶活性的抑制与模板引物(A)n·寡聚(dT)具有竞争性,这表明该药物可能与酶的模板引物结合位点相互作用。