title: Colocalization of Estrogen Receptors with the Fluorescent Tamoxifen Derivative, FLTX1, Analyzed by Confocal Microscopy.
abstract: Tamoxifen is a selective estrogen receptor modulator that competitively binds the ligand-binding domain of estrogen receptors. Binding of tamoxifen displaces its cognate ligand, 17β-estradiol, thereby hampering the activation of estrogen receptors. Cellular labeling of ER is typically carried out using specific antibodies which require permeabilization of cells, incubation with secondary antibodies, and are expensive and time consuming. In this article, we describe the usefulness of FLTX1, a novel fluorescent tamoxifen derivative, which allows the labeling of estrogen receptors in immunocytochemistry and immunohistochemistry studies, both under permeabilized and non-permeabilized conditions. Further, besides labeling canonical estrogen receptors, this novel fluorescent probe is also suitable for the identification of unconventional targets such membrane estrogen receptors as well as other noncanonical targets, some of which are likely responsible for the number of undesired side effects reported during long-term tamoxifen treatments.
authors.affiliation: Department of Physiology, Institute of Biomedical Technologies (ITB), Centre for Biomedical Research of the Canary Islands (CIBICAN), University of La Laguna, Tenerife, Spain.
authors.forename: Araceli
authors.initials: A
authors.lastname: Morales
authors.affiliation: Departamento de Fisiología, Facultad de Medicina, University of La Laguna, Tenerife, Spain.|Unidad asociada ULL-CSIC "Fisiología y biofísica de la membrana celular en patologías neurodegenerativas y tumorales, Tenerife, Spain.
authors.forename: Raquel
authors.initials: R
authors.lastname: Marín
authors.affiliation: Department of Animal Biology, University of La Laguna, Tenerife, Spain.
authors.forename: Jorge
authors.initials: J
authors.lastname: Marrero-Alonso
authors.affiliation: Instituto de Productos Naturales (IPNA, CSIC), Tenerife, Spain.|Unidad asociada ULL-CSIC "Fisiología y biofísica de la membrana celular en patologías neurodegenerativas y tumorales", Tenerife, Spain.
authors.forename: Alicia
authors.initials: A
authors.lastname: Boto
authors.affiliation: Laboratorio de Fisiología y Biofísica de Membranas, Departamento de Biología Animal, Facultad de Biología, University of La Laguna, Tenerife, Spain. madiaz@ull.es.|Unidad asociada ULL-CSIC "Fisiología y biofísica de la membrana celular en patologías neurodegenerativas y tumorales", Tenerife, Spain. madiaz@ull.es.
authors.forename: Mario
authors.initials: M
authors.lastname: Díaz
mesh_terms: D000818:Animals; D005260:Female; D005456:Fluorescent Dyes / Q000378:metabolism*; D006801:Humans; D061986:MCF-7 Cells; D051379:Mice; D018613:Microscopy, Confocal; D008856:Microscopy, Fluorescence; D010069:Oxadiazoles / Q000378:metabolism*; D011485:Protein Binding; D011960:Receptors, Estrogen / Q000378:metabolism*; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000378:metabolism; D014599:Uterus / Q000378:metabolism*; D057188:Workflow
chemical_list: D005456:Fluorescent Dyes; C000590551:N-(7-nitrobenzo(c)(1,2,5)oxadiazol-4-yl)demethyltamoxifen; D010069:Oxadiazoles; D011960:Receptors, Estrogen; D013629:Tamoxifen
keywords: Confocal microscopy; Estrogen receptor s; FLTX1; Fluorescent tamoxifen derivative; Intracellular estrogen receptor s; Membrane estrogen receptor s