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Further Characterization of Specific Drug Binding Sites on Human Serum Albumin
Abstract
The fluorescent probes 5-dimethylaminonaphthalene-1-sulfonamide and dansylsarcosine function as specific markers for two distinct binding sites for anionic drugs on human serum albumin (HSA). The binding of drugs to site I or II was detected by measuring the displacement of these probes. The results give an indication of some of the structural features required for binding at these sites. Stearic acid binding to HSA induced different conformational changes in the albumin at sites I and II, which were detected by changes in the fluorescence and/or strength of binding of probes specific for the two sites. This provides further evidence for qualitative differences between the two sites. The specificity of the sites for particular drugs, even at high drug to albumin ratios, was established, and the specificity and characteristics of the two sites on human adult and neonatal sera were shown to be similar to those on crystalline HSA.
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Cited by
Structural Basis of the Drug-binding Specificity of Human Serum Albumin
Ghuman, J., Zunszain, P. A., Petitpas, I., Bhattacharya, A. A., Otagiri, M., & Curry, S. (2005) · Journal of Molecular Biology · doi:10.1016/j.jmb.2005.07.075 · Cited by 1,941
The glycation of albumin: Structural and functional impacts
Rondeau, P., & Bourdon, E. (2011) · Biochimie · doi:10.1016/j.biochi.2010.12.003 · Cited by 433
Serum albumin in health and disease: esterase, antioxidant, transporting and signaling properties
Belinskaia, D. A., Voronina, P. A., Shmurak, V. I., Jenkins, R. O., & Goncharov, N. V. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms221910318 · Cited by 416
Current issues in measurement and reporting of urinary albumin excretion
Miller, W. G., Bruns, D. E., Hortin, G. L., Sandberg, S., Aakre, K. M., McQueen, M. J., Itoh, Y., Lieske, J. C., Seccombe, D. W., Jones, G., et al. (2009) · Clinical Chemistry · doi:10.1373/clinchem.2008.106567 · Cited by 381
Interactive Association of Drugs Binding to Human Serum Albumin
Yang, F., Zhang, Y., & Liang, H. (2014) · International Journal of Molecular Sciences · doi:10.3390/ijms15033580 · Cited by 376
Metadata
- Authors
- SUDLOW, G., BIRKETT, D. J., & WADE, D. N.
- Venue
- Molecular Pharmacology
- Publisher
- Elsevier BV
- Published
- 1976-11
- Volume
- 12
- Issue
- 6
- Pages
- 1052-1061
- ISSN
- 0026-895X (ISSN-L)
- OpenAlex
- W2324955203
- Cited by
- 1,443
- References
- 0
- FWCI
- 1.24
- Type
- journal article
- Language
- en
- Open access
- closed
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- SUDLOW, G., BIRKETT, D. J., & WADE, D. N. (1976). Further Characterization of Specific Drug Binding Sites on Human Serum Albumin. Molecular Pharmacology. https://doi.org/10.1016/s0026-895x(25)10855-9
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