title: Selective Estrogen Receptor Modulators and the Tissue-Selective Estrogen Complex: Analysis of Cell Type-Specific Effects Using In Vivo Imaging of a Reporter Mouse Model.
abstract: Selective estrogen receptor modulators (SERMs) are a class of compounds that act differentially on the estrogen receptor (ER) in various tissues with a mixed agonist/antagonistic activity (agonistic in some tissues while antagonist in others). This peculiarity represents a challenge for developing new hormone replacement therapies (HRTs) and highlights the need of new tools to evaluate the specific effects of a given SERM in different organs/tissues of an entire organism and with time. Reporter mice represent invaluable tools in pharmacology to analyze specific signaling in physiological conditions and monitor the effects of drugs acting on these signals in a spatio-temporal dimension. Here, we describe an in vivo protocol to examine the effects of different SERMs on estrogen receptor activity by using the ERE-Luc reporter model, a mouse that reports ER transcriptional activity.
authors.affiliation: Center of Excellence on Neurodegenerative Diseases and Department of Pharmacological and Biomolecular Sciences, University of Milan, via Balzaretti 9, 20133, Milan, Italy. sara.dellatorre@unimi.it.
authors.forename: Sara
authors.initials: S
authors.lastname: Della Torre
authors.affiliation: Center of Excellence on Neurodegenerative Diseases and Department of Pharmacological and Biomolecular Sciences, University of Milan, via Balzaretti 9, 20133, Milan, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Ciana
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D005260:Female; D005786:Gene Expression Regulation; D017930:Genes, Reporter; D049409:Luciferases, Firefly / Q000096:biosynthesis* / Q000235:genetics; D008163:Luminescent Measurements; D008810:Mice, Inbred C57BL; D008822:Mice, Transgenic; D057054:Molecular Imaging / Q000379:methods*; D010052:Ovariectomy; D020218:Response Elements / Q000187:drug effects*; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology*; D013997:Time Factors; D014158:Transcription, Genetic / Q000187:drug effects; D057188:Workflow
chemical_list: D020845:Selective Estrogen Receptor Modulators; D049409:Luciferases, Firefly
keywords: Clustering analysis; Estrogen receptors; In vivo imaging; Longitudinal studies; Luciferase; Reporter mice; Selective estrogen receptor modulators (SERMs)