Abstract:
Class B G protein-coupled receptors (GPCRs) are involved in a variety of human pathophysiological states. These groups of membrane receptors are less studied than class A GPCRs due to the lack of structural information, delayed small molecule drug discovery, and scarce fluorescence detection tools available. The class B corticotropin-releasing hormone type 1 receptor (CRHR1) is a key player in the stress response whose dysregulation is critically involved in stress-related disorders: psychiatric conditions (i.e. depression, anxiety, and addictions), neuroendocrinological alterations, and neurodegenerative diseases. Here, we present a strategy to label GPCRs with a small fluorescent antagonist that permits the observation of the receptor in live cells through stochastic optical reconstruction microscopy (STORM) with 23 nm resolution. The marker, an aza-BODIPY derivative, was designed based on computational docking studies, then synthesized, and finally tested in biological cells. Experiments on hippocampal neurons demonstrate antagonist effects in similar concentrations as the well-established antagonist CP-376395. A quantitative analysis of two color STORM images enabled the determination of the binding affinity of the new marker in the cellular environment. This journal is © the Owner Societies.
Registro:
Documento: |
Artículo
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Título: | A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells |
Autor: | Szalai, A.M.; Armando, N.G.; Barabas, F.M.; Stefani, F.D.; Giordano, L.; Bari, S.E.; Cavasotto, C.N.; Silberstein, S.; Aramendía, P.F. |
Filiación: | Centro de Investigaciones en Bionanociencias-Elizabeth Jares-Erijman (CIBION), CONICET, Godoy Cruz 2390, Ciudad de Buenos Aires, 1425, Argentina Departamento de Química Inorgánica Analítica y Química Física, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, Ciudad de Buenos Aires, 1428, Argentina Instituto de Investigación en Biomedicina de Buenos Aires (IBioBA), CONICET, Partner Institute of the Max Planck Society, Godoy Cruz 2390, Bernal, Provincia de Buenos Aires, 1425, Argentina Departamento de Ciencia y Tecnología, Universidad Nacional de Quilmes, Roque Sáenz Peña 352, Bernal, Provincia de Buenos Aires, 1876, Argentina Departamento de Física, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 1, Buenos Aires, 1428, Argentina Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, Ciudad de Buenos Aires, 1428, Argentina Instituto de Química Física de Materiales, Medio Ambiente y Energía (INQUIMAE), CONICET-UBA, Ciudad Universitaria, Pabellón 2, Ciudad de Buenos Aires, 1428, Argentina Departamento de Fisiología, Biología Molecular y Celular, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, Ciudad de Buenos Aires, 1428, Argentina Science for Life Laboratory, KTH Royal Institute of Technology, Tomtebodavagen 23A, Stockholm, 171 65, Sweden Instituto de Investigaciones en Medicina Traslacional (IIMT), CONICET, Universidad Austral, Av. Presidente Peron 1500, Derqui-Pilar, B1629AHJ, Argentina
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Palabras clave: | biological marker; corticotropin releasing factor receptor; corticotropin releasing factor receptor 1; fluorescent dye; antagonists and inhibitors; chemical structure; chemistry; fluorescence imaging; fluorescence microscopy; human; molecular docking; nanotechnology; synthesis; Biomarkers; Fluorescent Dyes; Humans; Microscopy, Fluorescence; Molecular Docking Simulation; Molecular Structure; Nanotechnology; Optical Imaging; Receptors, Corticotropin-Releasing Hormone |
Año: | 2018
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Volumen: | 20
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Número: | 46
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Página de inicio: | 29212
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Página de fin: | 29220
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DOI: |
http://dx.doi.org/10.1039/c8cp06196c |
Título revista: | Physical Chemistry Chemical Physics
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Título revista abreviado: | Phys. Chem. Chem. Phys.
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ISSN: | 14639076
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CODEN: | PPCPF
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CAS: | Biomarkers; CRF receptor type 1; Fluorescent Dyes; Receptors, Corticotropin-Releasing Hormone
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Registro: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14639076_v20_n46_p29212_Szalai |
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Citas:
---------- APA ----------
Szalai, A.M., Armando, N.G., Barabas, F.M., Stefani, F.D., Giordano, L., Bari, S.E., Cavasotto, C.N.,..., Aramendía, P.F.
(2018)
. A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells. Physical Chemistry Chemical Physics, 20(46), 29212-29220.
http://dx.doi.org/10.1039/c8cp06196c---------- CHICAGO ----------
Szalai, A.M., Armando, N.G., Barabas, F.M., Stefani, F.D., Giordano, L., Bari, S.E., et al.
"A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells"
. Physical Chemistry Chemical Physics 20, no. 46
(2018) : 29212-29220.
http://dx.doi.org/10.1039/c8cp06196c---------- MLA ----------
Szalai, A.M., Armando, N.G., Barabas, F.M., Stefani, F.D., Giordano, L., Bari, S.E., et al.
"A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells"
. Physical Chemistry Chemical Physics, vol. 20, no. 46, 2018, pp. 29212-29220.
http://dx.doi.org/10.1039/c8cp06196c---------- VANCOUVER ----------
Szalai, A.M., Armando, N.G., Barabas, F.M., Stefani, F.D., Giordano, L., Bari, S.E., et al. A fluorescence nanoscopy marker for corticotropin-releasing hormone type 1 receptor: Computer design, synthesis, signaling effects, super-resolved fluorescence imaging, and: In situ affinity constant in cells. Phys. Chem. Chem. Phys. 2018;20(46):29212-29220.
http://dx.doi.org/10.1039/c8cp06196c