阿非科林、膦甲酸和无环核苷三磷酸对疱疹病毒DNA聚合酶的相互排斥抑制作用。
Mutually exclusive inhibition of herpesvirus DNA polymerase by aphidicolin, phosphonoformate, and acyclic nucleoside triphosphates.
作者信息
Frank K B, Cheng Y C
出版信息
Antimicrob Agents Chemother. 1985 Apr;27(4):445-8. doi: 10.1128/AAC.27.4.445.
Abstract
Dual inhibitor studies were performed to examine the interaction of aphidicolin, phosphonoformate, 9-(2-hydroxyethoxymethyl)guanine triphosphate, and 9-(1,3-dihydroxy-2-propoxymethyl)guanine triphosphate with herpes simplex virus DNA polymerase. Kinetic data indicated that inhibition by one agent prevents simultaneous inhibition by a second agent, producing a mutually exclusive inhibition pattern. This suggested that binding sites on the DNA polymerase molecule for these compounds are kinetically overlapping. These findings should be taken into consideration for the design of future antiviral compounds and combination chemotherapy protocols.
摘要
进行了双重抑制剂研究，以检测阿非科林、膦甲酸、9-(2-羟乙氧基甲基)鸟嘌呤三磷酸和9-(1,3-二羟基-2-丙氧基甲基)鸟嘌呤三磷酸与单纯疱疹病毒DNA聚合酶的相互作用。动力学数据表明，一种药物的抑制作用会阻止第二种药物同时产生抑制作用，从而产生相互排斥的抑制模式。这表明这些化合物在DNA聚合酶分子上的结合位点在动力学上是重叠的。在设计未来的抗病毒化合物和联合化疗方案时应考虑到这些发现。
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