title: A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER).
abstract: We report the rational design, based on docking simulations, and synthesis of the first fluorescent and selective probe of GPER for bioimaging purposes and functional dissecting studies. It has been conceived as a Bodipy derivative and obtained by accessible and direct synthesis. Its optical properties have been measured in different solvents, showing insensitivity to their polarity. Its binding to GPER was achieved by competition assays with [3H]E2 and [5,6-3H] nicotinic acid in ER-negative and GPER-positive SkBr3 breast cancer cells. SkBr3 cells, transfected with a GPER expression vector containing a FLAG tag, were used to confirm that the fluorophore binds to GPER in a specific manner.
authors.affiliation: Department of "Scienze del Farmaco e Prodotti per la Salute", v. Annunziata, Università degli Studi di Messina, Polo Universitario, 98168 Messina, Italy.
authors.forename: T
authors.initials: T
authors.lastname: Papalia
authors.forename: R
authors.initials: R
authors.lastname: Lappano
authors.forename: A
authors.initials: A
authors.lastname: Barattucci
authors.forename: A
authors.initials: A
authors.lastname: Pisano
authors.forename: G
authors.initials: G
authors.lastname: Bruno
authors.forename: M F
authors.initials: MF
authors.lastname: Santolla
authors.forename: S
authors.initials: S
authors.lastname: Campagna
authors.forename: P
authors.initials: P
authors.lastname: De Marco
authors.forename: F
authors.initials: F
authors.lastname: Puntoriero
authors.forename: E M
authors.initials: EM
authors.lastname: De Francesco
authors.forename: C
authors.initials: C
authors.lastname: Rosano
authors.forename: M
authors.initials: M
authors.lastname: Maggiolini
authors.forename: P
authors.initials: P
authors.lastname: Bonaccorsi
mesh_terms: D001665:Binding Sites; D001896:Boron Compounds / Q000737:chemistry*; D002478:Cells, Cultured; D002623:Chemistry Techniques, Analytical / Q000295:instrumentation / Q000379:methods*; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D043562:Receptors, G-Protein-Coupled / Q000032:analysis*
chemical_list: C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D005456:Fluorescent Dyes; D043562:Receptors, G-Protein-Coupled