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用于表征HAS上两个特异性药物结合位点的荧光探针

人血清白蛋白(HSA)上有两个主要的结合位点(I: 蓝，II: 黄)与各种药物结合，其会对药代动力学和药理作用发挥重大影响。荧光探针丹酰胺 (1)和丹磺酰甘氨酸 (2)可以选择性的分别与位点I和II相互作用^1,2)。BD140 (3)也可以特异性的与药物结合位点II结合³⁾。荧光滴定分析发现，由于药物的竞争取代，探针的荧光发生了变化。通过这些试剂取代荧光探针的模式可以识别两个特异性药物结合位点，因此，这些试剂可用于HSA上结合位点的表征。

D4898,D5405,D5406

关键词:
D5405 丹酰胺 [1431-39-6]
D5406 丹磺酰甘氨酸 [1091-85-6]
D4898 BD140 [1201643-08-4]

文献

1)The Characterization of Two Specific Drug Binding Sites on Human Serum Albumin
- G. Sudlow, D. J. Birkett, D. N. Wade, Mol. Pharmacol. 1975, 11, 824.
2)Further Characterization of Specific Drug Binding Sites on Human Serum Albumin
- G. Sudlow, D. J. Birkett And D. N. Wade, Mol. Pharmacol. 1976, 12, 1052.
3)Fluorescent Dye Cocktail for Multiplex Drug-Site Mapping on Human Serum Albumin
- J. C. Er, M. Vendrell, M. K. Tang, D. Zhai, Y.-T. Chang, ACS Comb. Sci. 2013, 15, 452.