title: Rapid on-line profiling of estrogen receptor binding metabolites of tamoxifen.
abstract: Here we present a high-resolution screening (HRS) methodology for postcolumn on-line profiling of metabolites with affinity for the estrogen receptor alpha (ERalpha). Tamoxifen, which is metabolized into multiple metabolites, was used as the model compound. Most of the 14 metabolites detected exhibited affinity for the ERalpha. The HRS methodology shows great potential for metabolite bio-affinity profiling and application in drug discovery and development.
authors.affiliation: Leiden Amsterdam Center for Drug Research/Division of Molecular Toxicology, Department of Chemistry and Pharmacochemistry, Vrije Universiteit, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.
authors.forename: Jeroen
authors.initials: J
authors.lastname: Kool
authors.forename: Rawi
authors.initials: R
authors.lastname: Ramautar
authors.forename: Sebastiaan M
authors.initials: SM
authors.lastname: van Liempd
authors.forename: Joran
authors.initials: J
authors.lastname: Beckman
authors.forename: Frans J J
authors.initials: FJ
authors.lastname: de Kanter
authors.forename: John H N
authors.initials: JH
authors.lastname: Meerman
authors.forename: Tim
authors.initials: T
authors.lastname: Schenk
authors.forename: Hubertus
authors.initials: H
authors.lastname: Irth
authors.forename: Jan N M
authors.initials: JN
authors.lastname: Commandeur
authors.forename: Nico P E
authors.initials: NP
authors.lastname: Vermeulen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism* / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid / Q000295:instrumentation; D004965:Estrogen Antagonists / Q000378:metabolism* / Q000493:pharmacokinetics; D047628:Estrogen Receptor alpha / Q000378:metabolism*; D066298:In Vitro Techniques; D008024:Ligands; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats; D021241:Spectrometry, Mass, Electrospray Ionization; D013552:Swine; D013629:Tamoxifen / Q000378:metabolism* / Q000493:pharmacokinetics
chemical_list: D000970:Antineoplastic Agents; D004965:Estrogen Antagonists; D047628:Estrogen Receptor alpha; D008024:Ligands; D013629:Tamoxifen