A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER)

T. Papalia; R. Lappano; A. Barattucci; A. Pisano; G. Bruno; M. F. Santolla; S. Campagna; P. De Marco; F. Puntoriero; E. M. De Francesco; C. Rosano; M. Maggiolini; P. Bonaccorsi

doi:10.1039/c5ob01827g

A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER)

T. Papalia, R. Lappano, A. Barattucci, A. Pisano, G. Bruno, M. F. Santolla, S. Campagna, P. De Marco, F. Puntoriero, E. M. De Francesco, C. Rosano, M. Maggiolini, P. Bonaccorsi

A.O.U. San Martino - IST, Istituto Nazionale Ricerca sul Cancro (GENOVA)

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	10437-10441
Number of pages	5
Journal	Organic and Biomolecular Chemistry
Volume	13
Issue number	42
DOIs	https://doi.org/10.1039/c5ob01827g
Publication status	Published - 2015

ASJC Scopus subject areas

Physical and Theoretical Chemistry
Organic Chemistry
Biochemistry

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Papalia, T., Lappano, R., Barattucci, A., Pisano, A., Bruno, G., Santolla, M. F., Campagna, S., De Marco, P., Puntoriero, F., De Francesco, E. M., Rosano, C., Maggiolini, M., & Bonaccorsi, P. (2015). A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER). Organic and Biomolecular Chemistry, 13(42), 10437-10441. https://doi.org/10.1039/c5ob01827g

Papalia, T, Lappano, R, Barattucci, A, Pisano, A, Bruno, G, Santolla, MF, Campagna, S, De Marco, P, Puntoriero, F, De Francesco, EM, Rosano, C, Maggiolini, M & Bonaccorsi, P 2015, 'A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER)', Organic and Biomolecular Chemistry, vol. 13, no. 42, pp. 10437-10441. https://doi.org/10.1039/c5ob01827g

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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.",

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T1 - A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER)

AU - Papalia, T.

AU - Lappano, R.

AU - Barattucci, A.

AU - Pisano, A.

AU - Bruno, G.

AU - Santolla, M. F.

AU - Campagna, S.

AU - De Marco, P.

AU - Puntoriero, F.

AU - De Francesco, E. M.

AU - Rosano, C.

AU - Maggiolini, M.

AU - Bonaccorsi, P.

PY - 2015

Y1 - 2015

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AB - 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.

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A Bodipy as a luminescent probe for detection of the G protein estrogen receptor (GPER)

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