title: Ligand fishing using new chitosan based functionalized Androgen Receptor magnetic particles.
abstract: Superparamagnetic nanoparticles with chemically modified chitosan has been proposed as a potential support for the immobilization of the androgen receptor (AR). The study involved comparison of different AR carriers like commercially available magnetic beads coated with silica (BcMag) and chitosan coated nanoparticles with different amount of amino groups. The immobilization was carried out through covalent immobilization of the AR through the terminal amino group or through available carboxylic acids. The initial characterization of the AR coated magnetic beads was carried out with dihydrotestosterone, a known AR ligand. Subsequently, chitosan modified nanporticles with long-distanced primary amino groups (Fe3O4CS-(NH2)3) (upto 8.34mM/g) were used for further study to isolate known AR ligands (bicalutamide, flutamide, hydroxyflutamide and levonogestrel) from a mixture of tested compounds in ammonium acetate buffer [10mM, pH 7.4]. The results showed that the selected nanoparticles are a promising semi-quantitative tool for the identification of high affinity compounds to AR and might be of special importance in the identification of novel agonists or antiandrogens.
authors.affiliation: Nicolaus Copernicus University in Torun, Ludwik Rydygier Collegium Medicum in Bydgoszcz, Department of Medicinal Chemistry, ul. Jurasza 2, 85-089 Bydgoszcz, Poland. Electronic address: mmars@cm.umk.pl.
authors.forename: Michał Piotr
authors.initials: MP
authors.lastname: Marszałł
authors.affiliation: Nicolaus Copernicus University in Torun, Ludwik Rydygier Collegium Medicum in Bydgoszcz, Department of Medicinal Chemistry, ul. Jurasza 2, 85-089 Bydgoszcz, Poland.
authors.forename: Wiktor Dariusz
authors.initials: WD
authors.lastname: Sroka
authors.affiliation: Nicolaus Copernicus University in Torun, Ludwik Rydygier Collegium Medicum in Bydgoszcz, Department of Medicinal Chemistry, ul. Jurasza 2, 85-089 Bydgoszcz, Poland.
authors.forename: Adam
authors.initials: A
authors.lastname: Sikora
authors.affiliation: Nicolaus Copernicus University in Torun, Faculty of Chemistry Gagarina 7, 87-100 Torun, Poland.
authors.forename: Dorota
authors.initials: D
authors.lastname: Chełminiak
authors.affiliation: Nicolaus Copernicus University in Torun, Faculty of Chemistry Gagarina 7, 87-100 Torun, Poland.
authors.forename: Marta
authors.initials: M
authors.lastname: Ziegler-Borowska
authors.affiliation: Nicolaus Copernicus University in Torun, Ludwik Rydygier Collegium Medicum in Bydgoszcz, Department of Medicinal Chemistry, ul. Jurasza 2, 85-089 Bydgoszcz, Poland.
authors.forename: Tomasz
authors.initials: T
authors.lastname: Siódmiak
authors.affiliation: Laboratory of Clinical Investigation, National Institute on Aging Intramural Research Program, National Institutes of Health, Baltimore, MD, USA.
authors.forename: Ruin
authors.initials: R
authors.lastname: Moaddel
mesh_terms: D000726:Androgen Antagonists / Q000378:metabolism*; D048271:Chitosan / Q000737:chemistry*; D055808:Drug Discovery / Q000379:methods*; D055767:Immobilized Proteins / Q000737:chemistry / Q000378:metabolism*; D008024:Ligands; D058185:Magnetite Nanoparticles / Q000737:chemistry*; D011485:Protein Binding; D011944:Receptors, Androgen / Q000737:chemistry / Q000378:metabolism*; D013499:Surface Properties
chemical_list: D000726:Androgen Antagonists; D055767:Immobilized Proteins; D008024:Ligands; D058185:Magnetite Nanoparticles; D011944:Receptors, Androgen; D048271:Chitosan
keywords: Androgen receptor; Antiandrogens; Chitosan; Ligand fishing; Magnetic beads