Development of a Screening Assay for Ligands to the Estrogen Receptor Based on Magnetic Microparticles and LC-MS.

Development of a Screening Assay for Ligands to the Estrogen Receptor Based on Magnetic Microparticles and LC-MS. Research Abstract Details 

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Development of a Screening Assay for Ligands to the Estrogen Receptor Based on Magnetic Microparticles and LC-MS. Abstract Text:

Yongsoo Choi,Richard B van Breemen,

A high throughput screening assay for the identification of ligands to pharmacologically significant receptors was developed based on magnetic particles containing immobilized receptors followed by liquid chromatography-mass spectrometry (LC-MS). This assay is suitable for the screening of complex mixtures such as botanical extracts. For proof-of-principle, estrogen receptor-alpha (ER-alpha) and ER-beta were immobilized on magnetic particles functionalized with aldehyde or carboxylic acid groups. Alternatively, biotinylated ER was immobilized onto streptavidin-derivatized magnetic particles. The ER that was immobilized using the streptavidin-biotin chemistry showed higher activity than that immobilized on aldehyde or carboxylic acid functionalized magnetic particles. Immobilized ER was incubated with extracts of Trifolium pratense L. (red clover) or Humulus lupulus L. (hops). As a control for non-specific binding, each botanical extract was incubated with magnetic particles containing no ER. After magnetic separation of the particles containing bound ligands from the unbound components in the extract, the particles were washed, ligands were released using methanol, and then the ligands were identified using LC-MS. The estrogens genistein and daidzein were identified in the red clover extract, and the estrogen 8-prenylnaringenin was identified in the hop extract. These screening results are consistent with those obtained using previous screening approaches.

Development of a Screening Assay for Ligands to the Estrogen Receptor Based on Magnetic Microparticles and LC-MS. Publishing Authors By Initials

Y Choi,RB van Breemen,

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Development of a Screening Assay for Ligands to the Estrogen Receptor Based on Magnetic Microparticles and LC-MS. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Combinatorial chemistry & high throughput screenin

VOLUME: 11

Page Numbers: 1-6

Journal Abbreviation: Comb. Chem. High Throughput Sc

ISSN: 1386-2073

DAY: 28

MONTH: Jan

YEAR: 2008

Development of a Screening Assay for Ligands to the Estrogen Receptor Based on Magnetic Microparticles and LC-MS. Information

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LANGUAGE: eng

NlmUniqueID: 9810948

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Grant and Affiliation Information for Development of a Screening Assay for Ligands to the Estrogen Receptor Based on Magnetic Microparticles and LC-MS.

AFFILIATION: UIC/NIH Center for Botanical Dietary Supplements Research, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois College of Pharmacy, 833 South Wood Street, Chicago, IL 60612, USA. Breemen@uic.edu.

Country: Netherlands

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MEDLINETA: Comb Chem High Throughput Scre

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