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19 p, 1.2 MB |
Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer
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Liu, Junke (University of Science and Technology, Wuhan, China) ;
Zhang, Zongyong (University of Science and Technology, Wuhan, China) ;
Moreno-Delgado, David (Université de Montpellier, France) ;
Dalton, James A. R (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Rovira, Xavier (Université de Montpellier, France) ;
Trapero, Ana (Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Barcelona) ;
Goudet, Cyril (Université de Montpellier, France) ;
Llebaria, Amadeu (Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Barcelona) ;
Giraldo, Jesús (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Yuan, Qilin (University of Science and Technology, Wuhan, China) ;
Rondard, Philippe (Université de Montpellier, France) ;
Huang, Siluo (University of Science and Technology, Wuhan, China) ;
Liu, Jianfeng (University of Science and Technology, Wuhan, China) ;
Pin, Jean-Philippe (Université de Montpellier, France) ;
Universitat Autònoma de Barcelona.
Departament de Pediatria, Obstetrícia i Ginecologia i de Medicina Preventiva i Salut Pública
GPCRs play critical roles in cell communication. Although GPCRs can form heteromers, their role in signaling remains elusive. Here we used rat metabotropic glutamate (mGlu) receptors as prototypical dimers to study the functional interaction between each subunit. [...]
2017 -  10.7554/eLife.26985
eLife, Vol. 6 (august 2017)
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33 p, 2.5 MB |
Pharmacological evidence for a metabotropic glutamate receptor heterodimer in neuronal cells
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Moreno Delgado, David (Universitat de Montpellier) ;
Møller, Thor C. (Universitat de Montpellier) ;
Ster, Jeanne (Universitat de Montpellier) ;
Giraldo, Jesús (Universitat Autònoma de Barcelona. Laboratori de Neurofarmacologia Molecular i Bioinformàtica) ;
Maurel, Damien (Universitat de Montpellier) ;
Rovira, Xavier (Universitat de Montpellier) ;
Scholler, Pauline (Universitat de Montpellier) ;
Zwier, Jurriaan M. (CisBio Bioassays, Codolet) ;
Perroy, Julie (Universitat de Montpellier) ;
Durroux, Thierry (Universitat de Montpellier) ;
Trinquet, Eric (CisBio Bioassays, Codolet) ;
Prezeau, Laurent (Universitat de Montpellier) ;
Rondard, Philippe (Universitat de Montpellier) ;
Pin, Jean-Philippe (Universitat de Montpellier)
Metabotropic glutamate receptors (mGluRs) are mandatory dimers playing important roles in regulating CNS function. Although assumed to form exclusive homodimers, 16 possible heterodimeric mGluRs have been proposed but their existence in native cells remains elusive. [...]
2017 - 10.7554/eLife.25233
eLife, Vol. 6 (june 2017)
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20 p, 2.1 MB |
Optical control of pain in vivo with a photoactive mGlu receptor negative allosteric modulator
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Font Inglès, Joan (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
López-Cano, Marc (Institut d'Investigació Biomèdica de Bellvitge) ;
Notartomaso, Serena (I.R.C.C.S. Neuromed, Pozzilli, Italy) ;
Scarselli, Pamela (I.R.C.C.S. Neuromed, Pozzilli, Italy) ;
Di Pietro, Paola (I.R.C.C.S. Neuromed, Pozzilli, Italy) ;
Bresolí-Obach, Roger (Universitat Ramon Llull. Institut Químic de Sarrià-IQS) ;
Battaglia, Giuseppe (I.R.C.C.S. Neuromed, Pozzilli, Italy) ;
Malhaire, Fanny (Université de Montpellier) ;
Rovira, Xavier (Université de Montpellier) ;
Catena, Juanlo (Institut de Química Avançada de Catalunya) ;
Giraldo, Jesús (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Pin, Jean-Philippe (Université de Montpellier) ;
Fernández-Dueñas, Víctor (Institut d'Investigació Biomèdica de Bellvitge) ;
Goudet, Cyril (Université de Montpellier) ;
Nonell, Santi (Universitat Ramon Llull. Institut Químic de Sarrià-IQS) ;
Nicoletti, Ferdinando (I.R.C.C.S. Neuromed, Pozzilli, Italy) ;
Llebaria, Amadeu (Institut de Química Avançada de Catalunya) ;
Ciruela, Francisco (Institut d'Investigació Biomèdica de Bellvitge)
Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i. e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type 5 (mGlu) receptor negative allosteric modulator raseglurant. [...]
2017 - 10.7554/eLife.23545
eLife, Vol. 6 (april 2017)
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11 p, 2.3 MB |
Illuminating phenylazopyridines to photoswitch metabotropic glutamate receptors : from the flask to the animals
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Gómez-Santacana, Xavier (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Pittolo, Silvia (Institut de Bioenginyeria de Catalunya) ;
Rovira, Xavier (Université de Montpellier. Institute of Functional Genomics) ;
Lopez, Marc (Universitat de Barcelona. Unitat de Farmacologia) ;
Zussy, Charleine (Université de Montpellier. Institute of Functional Genomics) ;
Dalton, James A. R.. (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Faucherre, Adèle (Université de Montpellier. Institute of Functional Genomics) ;
Jopling, Chris (Université de Montpellier. Institute of Functional Genomics) ;
Pin, Jean-Philippe (Université de Montpellier. Institute of Functional Genomics) ;
Ciruela, Francisco (Universitat de Barcelona. Unitat de Farmacologia) ;
Goudet, Cyril (Université de Montpellier. Institute of Functional Genomics) ;
Giraldo, Jesús (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Gorostiza, Pau (Institut de Bioenginyeria de Catalunya) ;
Llebaria, Amadeu (Institut de Química Avançada de Catalunya)
Phenylazopyridines are photoisomerizable compounds with high potential to control biological functions with light. We have obtained a series of phenylazopyridines with light dependent activity as negative allosteric modulators (NAM) of metabotropic glutamate receptor subtype 5 (mGlu). [...]
2017 - 10.1021/acscentsci.6b00353
ACS Central Science, Vol. 3, issue 1 (Jan. 2017) , p. 81-91
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24 p, 1.3 MB |
Shining Light On An mGlu5 Photoswitchable NAM : A Theoretical Perspective
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Dalton, James A. R.. (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Lans, Isaias (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Rovira Algans, Xavier (Institut de Génomique Fonctionnelle) ;
Malhaire, Fanny (Institut de Génomique Fonctionnelle) ;
Gómez-Santacana, Xavier (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Pittolo, Silvia (Institut de Bioenginyeria de Catalunya) ;
Gorostiza, Pau (Institut de Bioenginyeria de Catalunya) ;
Llebaria, Amadeu (Institut de Química Avançada de Catalunya) ;
Goudet, Cyril (Institut de Génomique Fonctionnelle) ;
Pin, Jean-Philippe (Institut de Génomique Fonctionnelle) ;
Giraldo, Jesús (Universitat Autònoma de Barcelona. Institut de Neurociències)
Metabotropic glutamate receptors (mGluRs) are important drug targets because of their involvement in several neurological diseases. Among mGluRs, mGlu5 is a particularly high-profile target because its positive or negative allosteric modulation can potentially treat schizophrenia or anxiety and chronic pain, respectively. [...]
2016 - 10.2174/1570159X13666150407231417
Current neuropharmacology, Vol. 14, Num. 5 (July 2016) , p. 441-454
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