Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs.

Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs. Research Abstract Details 

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Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs. Abstract Text:

Jianzhong Chen,David S Hage,

A new chromatographic method was developed for characterizing allosteric interactions between an immobilized binding agent and low-solubility compounds. This approach was illustrated by using it to characterize the interactions between tamoxifen and warfarin during their binding to the protein human serum albumin (HSA), with beta-cyclodextrin being employed as a solubilizing agent for these drugs. It was confirmed in this work through several experiments that warfarin had a single binding site on HSA with an association equilibrium constant of (2-5) x 10(5) M(-1) (average, 3.9 x 10(5) M(-1)) at 37 degrees C, in agreement with previous reports. It was also found that tamoxifen had a single major binding site on HSA, with an association equilibrium constant of (3-4) x 10(7) M(-1) (average, 3.5 x 10(7) M(-1)) at 37 degrees C. When warfarin was used as a mobile-phase additive in competition studies with tamoxifen, this had a positive allosteric effect on tamoxifen/HSA binding, giving a coupling constant of 2.3 (+/-0.3). Competitive studies using tamoxifen as a mobile-phase additive indicated that tamoxifen had a negative allosteric effect on warfarin/HSA binding, providing a coupling constant of 0.79 (+/-0.03). A unique feature of the technique described in this report was its ability to independently examine both directions of the warfarin/tamoxifen allosteric interaction. This approach is not limited to warfarin, tamoxifen, and HSA but can also be used to study other solutes and binding agents.

Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs. Publishing Authors By Initials

J Chen,DS Hage,

For similar polycyclic compounds: macrocyclic compounds: cyclodextrins: beta-cyclodextrins research abstracts see: polycyclic compounds: macrocyclic compounds: cyclodextrins: beta-cyclodextrins research

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Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Analytical chemistry

VOLUME: 78

Page Numbers: 2672-83

Journal Abbreviation: Anal. Chem.

ISSN: 0003-2700

DAY: 15

MONTH: Apr

YEAR: 2006

Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 370536

Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs. Keywords Mesh Terms:

KEYWORDS: beta-Cyclodextrins

MESH TERMS: chemistry

Chemical & Substance for Abstract: Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs. Information

Substance Name: Warfarin

Registry Number: 81-81-2

Grant and Affiliation Information for Quantitative studies of allosteric effects by biointeraction chromatography: analysis of protein binding for low-solubility drugs.

AFFILIATION: Department of Chemistry, University of Nebraska, Lincoln, Nebraska 68588-0304, USA.

Country: United States

AGENCY: United States NIGMS

GRANT: R01 GM044931

ACRONYM: GM

MEDLINETA: Anal Chem

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