2. Academic Validation
  3. Colocalization of Estrogen Receptors with the Fluorescent Tamoxifen Derivative, FLTX1, Analyzed by Confocal Microscopy

Colocalization of Estrogen Receptors with the Fluorescent Tamoxifen Derivative, FLTX1, Analyzed by Confocal Microscopy

  • Methods Mol Biol. 2016;1366:163-173. doi: 10.1007/978-1-4939-3127-9_13.
Araceli Morales 1,  Raquel Marín 2 3,  Jorge Marrero-Alonso 4,  Alicia Boto 5 6,  Mario Díaz 7 8
Affiliations

Affiliations

  • 1 Department of Physiology, Institute of Biomedical Technologies (ITB), Centre for Biomedical Research of the Canary Islands (CIBICAN), University of La Laguna, Tenerife, Spain.
  • 2 Departamento de Fisiología, Facultad de Medicina, University of La Laguna, Tenerife, Spain.
  • 3 Unidad asociada ULL-CSIC "Fisiología y biofísica de la membrana celular en patologías neurodegenerativas y tumorales, Tenerife, Spain.
  • 4 Department of Animal Biology, University of La Laguna, Tenerife, Spain.
  • 5 Instituto de Productos Naturales (IPNA, CSIC), Tenerife, Spain.
  • 6 Unidad asociada ULL-CSIC "Fisiología y biofísica de la membrana celular en patologías neurodegenerativas y tumorales", Tenerife, Spain.
  • 7 Laboratorio de Fisiología y Biofísica de Membranas, Departamento de Biología Animal, Facultad de Biología, University of La Laguna, Tenerife, Spain. madiaz@ull.es.
  • 8 Unidad asociada ULL-CSIC "Fisiología y biofísica de la membrana celular en patologías neurodegenerativas y tumorales", Tenerife, Spain. madiaz@ull.es.
PMID: 26585134 DOI: 10.1007/978-1-4939-3127-9_13
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.

Keywords

Confocal microscopy; Estrogen receptor s; FLTX1; Fluorescent tamoxifen derivative; Intracellular estrogen receptor s; Membrane estrogen receptor s.

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