Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembrane interface

Autor: Lei Liu, Zhiran Fan, Xavier Rovira, Li Xue, Salomé Roux, Isabelle Brabet, Mingxia Xin, Jean-Philippe Pin, Philippe Rondard, Jianfeng Liu

Publikováno v: eLife, Vol 10 (2021)

G protein-coupled receptors (GPCRs) are among the most promising drug targets. They often form homo- and heterodimers with allosteric cross-talk between receptor entities, which contributes to fine-tuning of transmembrane signaling. Specifically cont

Externí odkaz: https://doaj.org/article/637406475b8f4911855cad59cb27a13c

Nonclassical Ligand-Independent Regulation of Go Protein by an Orphan Class C G-Protein–Coupled Receptor

Autor: Jean-Philippe Pin, Mariana Hajj, Gilles Labesse, Laurent Prézeau, Claire Vol, Magali Cazade, Manuela Pastore, Jean-Charles Bologna, Teresa De Vita, Isabelle Brabet, Jaroslav Blahos, Charlotte Renassia

Publikováno v: Molecular Pharmacology. 96:233-246

The orphan G-protein-coupled receptor (GPCR) GPR158 is expressed in the brain, where it is involved in the osteocalcin effect on cognitive processes, and at the periphery, where it may contribute to glaucoma and cancers. GPR158 forms a complex with R

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6cbcad36e63a202d943f77dc4267fa8a
https://doi.org/10.1124/mol.118.113019

Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites

Autor: Amélie S. Tora, Sara Cesarini, Heather McLean, Cyril Goudet, Tiphanie Courtiol, Nadia Oueslati, Bruno Commare, Berin Karaman, Thomas Bessiron, Francine Acher, Frédéric R. Leroux, Isabelle A. Lemasson, Delphine Rigault, Laetitia Mony, Hugues-Olivier Bertrand, Jean-Philippe Pin, Isabelle McCort-Tranchepain, Anne Goupil-Lamy, Isabelle Brabet, Hervé Daniel, Françoise Colobert, Chelliah Selvam, Alexandre Cabayé

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2018, 61 (5), pp.1969-1989. ⟨10.1021/acs.jmedchem.7b01438⟩

This work was supported by the by the Fondation de France (comite Parkinson), the Agence Nationale de la Recherche (ANR-05-NEUR-0121-02, ANR-07-NEURO-047-04, and ANR-08-NEUR-006-02 in the frame of ERA-NET NEURON and ANR-13-BSV1-0006), the Fondation p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8135547c041835ec608d24f8a3198a92
https://hal.archives-ouvertes.fr/hal-02018007

Synthesis and Biological Evaluation of 1-Amino-2-Phosphonomethylcyclopropanecarboxylic Acids, New Group III Metabotropic Glutamate Receptor Agonists

Autor: Cyril Goudet, Hugues-Olivier Bertrand, Isabelle Brabet, Michael J. Marino, Pauline Sibille, Florence Gaven, Sébastien Lopez, Jacques Neyton, Jean-Philippe Pin, Ornella Valenti, Francine Acher, Nadia Oueslati, Marianne Amalric

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (15), pp.3585-95. ⟨10.1021/jm070262c⟩
Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (15), pp.3585-95. 〈10.1021/jm070262c〉
Journal of Medicinal Chemistry, 2007, 50 (15), pp.3585-95. ⟨10.1021/jm070262c⟩

International audience; Stereoisomers of 1-amino-2-phosphonomethylcyclopropanecarboxylic acid (APCPr), conformationally restricted analogues of L-AP4 (2-amino-4-phosphonobutyric acid), have been prepared and evaluated at recombinant group III metabot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1bd7047c1a9b87b58e5e71873c12613
https://doi.org/10.1021/jm070262c

Determination of the absolute configuration of phosphinic analogues of glutamate

Autor: Pascal Roussel, Frédéric R. Leroux, Delphine Rigault, Alain Tomas, Françoise Colobert, Isabelle A. Lemasson, Isabelle Brabet, Jean-Philippe Pin, Cyril Goudet, Bruno Commare, Patrick Deschamps, Francine Acher

Publikováno v: Organic and Biomolecular Chemistry
Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2015, 13 (4), pp.1106-1112. ⟨10.1039/C4OB01960A⟩
Organic & Biomolecular Chemistry
Organic & Biomolecular Chemistry, 2015, 13 (4), pp.1106-1112. ⟨10.1039/C4OB01960A⟩

A series of phosphinic glutamate derivatives (e.g.LSP1-2111) have been proven to be potent agonists of metabotropic glutamate (mGlu) receptors and shown promising in vivo activity. However, so far all were synthesized and tested as a mixture of two d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::338ce19f3a754855a76ed947a7cdba39
https://hal.archives-ouvertes.fr/hal-02268872