Choudhury G G, Banerjee A, Bhattacharyya B, Biswas B B
FEBS Lett. 1983 Sep 5;161(1):55-9. doi: 10.1016/0014-5793(83)80729-7.
Binding of two colchicine analogues, desacetamidocolchicine and 2-methoxy-5-(2',3',4'-trimethoxyphenyl) tropone to purified tubulin have been studied. Both analogues bind to tubulin with a significant increase in fluorescence polarization of the drugs in solutions containing tubulin. The Kd for tubulin-drug complexes were found to be 1.25 X 10(-6) M and 1.08 X 10(-6) M for desacetamidocolchicine and 2-methoxy-5-(2',3',4'-trimethoxyphenyl) tropone, respectively. Scatchard analysis of the fluorescence titration curve of drug tubulin interaction also gives the values of stoichiometry and affinity constant. These were 0.8 and 1.6 X 10(6) M-1 for desacetamidocolchicine, and 0.9 and 0.58 X 10(6) M-1 for 2-methoxy-5-(2',3',4'-trimethoxyphenyl) tropone.
已经研究了两种秋水仙碱类似物，去乙酰氨基秋水仙碱和2-甲氧基-5-（2'，3'，4'-三甲氧基苯基）色原酮与纯化微管蛋白的结合。在含有微管蛋白的溶液中，两种类似物均与微管蛋白结合，药物的荧光偏振显著增加。去乙酰氨基秋水仙碱和2-甲氧基-5-（2'，3'，4'-三甲氧基苯基）色原酮与微管蛋白 - 药物复合物的解离常数（Kd）分别为1.25×10^(-6) M和1.08×10^(-6) M。对药物与微管蛋白相互作用的荧光滴定曲线进行Scatchard分析，也得出了化学计量值和亲和常数。去乙酰氨基秋水仙碱的这些值分别为0.8和1.6×10^6 M^(-1)，2-甲氧基-5-（2'，3'，4'-三甲氧基苯基）色原酮的这些值分别为0.9和0.58×10^6 M^(-1)。
