微分绑定丙吡胺和华法林对映体对人类α(1)酸性糖蛋白变异。

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中川T, Kishino年代,伊藤,同样是十六米,宫崎骏K

微分绑定丙吡胺和华法林对映体对人类α(1)酸性糖蛋白变异。

Br中国新药杂志。2003;12月56 (6):664 - 9。

PubMed ID

14616427 (在PubMed

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目的:f1和遗传变异的alpha1-acid糖蛋白(亚美大陆煤层气有限公司)在各种生理和病理条件下改变。他们在他们的药物结合能力也有所不同。我们学习了亚美大陆煤层气有限公司的每个变量的立体选择绑定能力利用丙吡胺对映体(DP)和华法林(WR)。方法:亚美大陆煤层气有限公司变种被羟磷灰石层析分离。药物对映体的绑定亚美大陆煤层气有限公司Hummel-Dreyer变异研究的方法。绑定活动的特点被Scatchard情节分析检查。前五个伴氨基酸(112 - 116)残留的溴化氰(CNBr)片段(残留112 - 181)每个分开的亚美大陆煤层气有限公司分数被埃德曼降解阐明。结果:商业亚美大陆煤层气有限公司分为两个主要部分。残留112 - 116的分数相同的氨基酸序列预测亚美大陆煤层气有限公司基因,LAFDV,对f1变体编码。在分数3中,推导出的氨基酸序列亚美大陆煤层气有限公司B基因,FGSYL,成立,编码一个变种。 The binding affinities of both DP enantiomers in fraction 3 were significantly higher than those in fraction 2. The differences between dissociation constants (Kd) in fractions 2 and 3 were 5.2-fold for (S)-DP (P < 0.05) and 3.7-fold for (R)-DP (P < 0.001). The dissociation constant of (S)-DP (0.39 +/- 0.08 micro m) was lower than that of (R)-DP (0.53 +/- 0.10 micro m) in fraction 3 [95% confidence interval (CI) - 0.282, - 0.010; P < 0.05], although the binding activities of the DP enantiomers were almost the same in fraction 2. By contrast WR enantiomers had a higher binding affinity in fraction 2 than in fraction 3, the differences in dissociation constants between fractions 2 and 3 being 12.6-fold for (S)-WR (P < 0.001) and 8.3-fold for (R)-WR (P < 0.001). The dissociation constant of (S)-WR (0.28 +/- 0.10 microm) was significantly lower than that of (R)-WR (0.48 +/- 0.08 microm) in fraction 2 (95% CI - 0.369, - 0.028; P < 0.05), but there were no significant differences between the binding activities of WR enantiomers in fraction 3. CONCLUSIONS: DP and WR enantiomers bind preferentially to fraction 3 and fraction 2, respectively. Fractions 2 and 3 are encoded by the AAG A and the AAG B genes, respectively.

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药物载体

药物	航空公司	类	生物	药理作用	行动
丙吡胺	Alpha-1-acid糖蛋白1	蛋白质	人类	没有	其他/未知	细节
华法令阻凝剂	Alpha-1-acid糖蛋白1	蛋白质	人类	没有	不可用	细节