TITLE

Determination of drug–serum protein interactions via fluorescence polarization measurements

AUTHOR(S)
Mathias, Ulf; Jung, Manfred
PUB. DATE
July 2007
SOURCE
Analytical & Bioanalytical Chemistry;Jul2007, Vol. 388 Issue 5/6, p1147
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
New fast methods for the determination of pharmacokinetic behaviour of potential drug candidates are receiving increasing interest. We present a new homogeneous method for the determination of drug binding and drug competition for human serum albumin and α1-acid glycoprotein that is amenable to high-throughput-screening. It is based on selective fluorescent probes and the measurement of fluorescence polarization. This leads to decreased interference with fluorescent drugs as compared with previously published methods based on similar probes and the measurement of fluorescence intensity. The binding of highly fluorescent drugs that still interfere with the probes can be measured by simply titrating the drugs in a two-component system with the serum protein. The assay may also be used to discover strongly binding protein ligands that are interesting for drug-targeting strategies. Additionally, binding data could be obtained from larger libraries of compounds for in silico predictive pharmacokinetics. [Figure not available: see fulltext.]
ACCESSION #
25603351

 

Related Articles

  • Structure of molecular associates of fluorescent probes in solutions of human serum albumin. Buharova, E. M.; Vlasova, I. M.; Saletsky, A. M. // Journal of Applied Spectroscopy;Nov2008, Vol. 75 Issue 6, p785 

    Spectral-luminescent characteristics and molecular association processes in solutions of human serum albumin are analyzed at different pH values for three fluorescent probes (eosin, erythrosin, and fluorescein). Common features for all three probes in protein solutions are quenching of the...

  • Albumin-stabilized gold nanoclusters as viable fluorescent probes in non-titrimetric iodometry for the detection of oxidizing analytes. Li, Ruiping; Xu, Pingping; Tu, Yifeng; Yan, Jilin // Microchimica Acta;Jan2016, Vol. 183 Issue 1, p497 

    We describe a simple method for non-titrimetric determination of oxidative species capable of oxidizing iodide to form free iodine. The combined action of iodine and excess iodide leads to the etching of gold nanoclusters stabilized with serum albumin. The extent of fluorescence quenching...

  • In Silico Prediction of Interactions between Site II on Human Serum Albumin and Profen Drugs. Hideto Isogai; Noriaki Hirayama // ISRN Pharmaceutics;2013, p1 

    Since binding of a drug molecule to human serum albumin (HSA) significantly affects the pharmacokinetics of the drug, it is highly desirable to predict the binding affinity of the drug. Profen drugs are a widely used class of nonsteroidal anti-inflammatory drugs and it has been reported that...

  • Stereoselective binding of chiral drugs to plasma proteins. Shen, Qi; Wang, Lu; Zhou, Hui; Jiang, Hui-di; Yu, Lu-shan; Zeng, Su // Acta Pharmacologica Sinica;Aug2013, Vol. 34 Issue 8, p998 

    Chiral drugs show distinct biochemical and pharmacological behaviors in the human body. The binding of chiral drugs to plasma proteins usually exhibits stereoselectivity, which has a far-reaching influence on their pharmacological activities and pharmacokinetic profiles. In this review, the...

  • Towards the interaction mechanism of tocopherols and tocotrienols (vitamin E) with selected metabolizing enzymes. Upadhyay, Jyoti; Misra, Krishna // Bioinformation;2009, Vol. 3 Issue 8, p326 

    Vitamin E is a mixture of eight compounds α, β, γ, δ- tocopherols and α, β, γ, δ- tocotrienols. Their individual role in cellular transport as antioxidants and in metabolic pathways has been highlighted in the present work. All the eight compounds have been docked with...

  • Fluorescence nanoscopy by polarization modulation and polarization angle narrowing. Hafi, Nour; Grunwald, Matthias; van den Heuvel, Laura S; Aspelmeier, Timo; Chen, Jian-Hua; Zagrebelsky, Marta; Schütte, Ole M; Steinem, Claudia; Korte, Martin; Munk, Axel; Walla, Peter J // Nature Methods;May2014, Vol. 11 Issue 5, p579 

    When excited with rotating linear polarized light, differently oriented fluorescent dyes emit periodic signals peaking at different times. We show that measurement of the average orientation of fluorescent dyes attached to rigid sample structures mapped to regularly defined (50 nm)2 image...

  • Luminescent spectral properties of rhodamine derivatives while binding to serum albumin. Nizomov, N.; Ismailov, Z. F.; Kurtaliev, É. N.; Nizamov, Sh. N.; Khodzhaev, G.; Patsenker, L. D. // Journal of Applied Spectroscopy;May2006, Vol. 73 Issue 3, p432 

    We have studied the effect of blood serum albumin on the absorption and fluorescence spectra of rhodamine C (RC), rhodamine 6G (R6G), and rhodamine 3B (R3B). Interaction of the dye with protein is assessed using the binding parameters: binding constants and concentrations of binding sites. We...

  • Study of protein coatings cross-linked via the free-radical mechanism on magnetic nanoparticles by the method of spectral and fluorescent probes. Bychkova, A.; Pronkin, P.; Sorokina, O.; Tatikolov, A.; Rosenfeld, M. // Colloid Journal;Jul2014, Vol. 76 Issue 4, p387 

    Magnetite nanoparticles have been obtained with stable coatings formed from bovine and human serum albumins. The coatings are fixed by free-radical cross-linking of the proteins with the use of their ability to form interchain covalent bonds under the action of free radicals, which are generated...

  • Galectin Binding to Neo-Glycoproteins: LacDiNAc Conjugated BSA as Ligand for Human Galectin-3. Böcker, Sophia; Laaf, Dominic; Elling, Lothar // Biomolecules (2218-273X);2015, Vol. 5 Issue 3, following p1671 

    Carbohydrate-lectin interactions are relatively weak. As they play an important role in biological recognition processes, multivalent glycan ligands are designed to enhance binding affinity and inhibitory potency. We here report on novel neo-glycoproteins based on bovine serum albumin as...

Share

Read the Article

Courtesy of THE LIBRARY OF VIRGINIA

Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics