Kumar S A, Krakow J S
J Biol Chem. 1977 Aug 25;252(16):5724-8.
Cibacron blue F3GA is a potent inhibitor of the Azotobacter vinelandii DNA-directed RNA polymerase. Addition of 8 micrometer Cibacron blue F3GA prior to initiation results in a greater than 90% inhibition of the poly[d(A-T]-directed synthesis of poly[r(A-U)] while addition of the dye during the course of the reaction is without effect on chain elongation. Binding of RNA polymerase to [3H]poly[d(A-T)] is inhibited by only 15% in the presence of 8 micrometer Cibacron blue F3GA. Inhibition by Cibacron blue F3GA is noncompetitive with regard to ATP, UTP, or template. The poly[d(A-T)]-directed pyrophosphate exchange reaction is relatively resistant to inhibition by Cibacron blue F3GA. Rifampicin added to a similar reaction (in the presence of absence of Cibacron blue F3GA) results in 95% inhibition of the exchange reaction. The interaction of the RNA polymerase core enzyme with Cibacron blue F3GA is shown by the formation of a difference spectrum with a positive maximum at 675 nm which is not affected by the presence of a high concentration (4 micrometer) of rafampicin. The data indicate that Cibacron blue F3GA acts by binding to RNA polymerase and inhibits a step between the synthesis of the initial phosphodiester bond and formation of a stable ternary elongation complex.
汽巴克隆蓝F3GA是维涅兰德固氮菌DNA指导的RNA聚合酶的一种强效抑制剂。在起始反应前加入8微摩尔的汽巴克隆蓝F3GA会导致聚[r(A-U)]的聚[d(A-T)]指导合成受到超过90%的抑制,而在反应过程中加入该染料对链延伸没有影响。在8微摩尔汽巴克隆蓝F3GA存在的情况下,RNA聚合酶与[3H]聚[d(A-T)]的结合仅被抑制15%。汽巴克隆蓝F3GA的抑制作用在ATP、UTP或模板方面是非竞争性的。聚[d(A-T)]指导的焦磷酸交换反应对汽巴克隆蓝F3GA的抑制相对具有抗性。添加到类似反应中(无论是否存在汽巴克隆蓝F3GA)的利福平会导致交换反应受到95%的抑制。RNA聚合酶核心酶与汽巴克隆蓝F3GA的相互作用通过在675纳米处形成一个正最大吸收峰的差示光谱来显示,该光谱不受高浓度(4微摩尔)利福平存在的影响。数据表明,汽巴克隆蓝F3GA通过与RNA聚合酶结合起作用,并抑制初始磷酸二酯键合成与稳定三元延伸复合物形成之间的一个步骤。