Literature DB >> 25173999

An allosteric modulator to control endogenous G protein-coupled receptors with light.

Silvia Pittolo1, Xavier Gómez-Santacana2, Kay Eckelt3, Xavier Rovira4, James Dalton5, Cyril Goudet6, Jean-Philippe Pin6, Artur Llobet7, Jesús Giraldo5, Amadeu Llebaria8, Pau Gorostiza9.   

Abstract

Controlling drug activity with light offers the possibility of enhancing pharmacological selectivity with spatial and temporal regulation, thus enabling highly localized therapeutic effects and precise dosing patterns. Here we report on the development and characterization of what is to our knowledge the first photoswitchable allosteric modulator of a G protein-coupled receptor. Alloswitch-1 is selective for the metabotropic glutamate receptor mGlu5 and enables the optical control of endogenous mGlu5 receptors.

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Year:  2014        PMID： 25173999     DOI： 10.1038/nchembio.1612

Source DB:  PubMed          Journal:  Nat Chem Biol        ISSN： 1552-4450            Impact factor:   15.040


  31 in total

Review 1.  Light- and drug-activated G-protein-coupled receptors to control intracellular signalling.

Authors:  Olivia A Masseck; Johanna M Rubelowski; Katharina Spoida; Stefan Herlitze
Journal:  Exp Physiol       Date:  2010-11-01       Impact factor: 2.969

2.  Light-regulated stapled peptides to inhibit protein-protein interactions involved in clathrin-mediated endocytosis.

Authors:  Laura Nevola; Andrés Martín-Quirós; Kay Eckelt; Núria Camarero; Sébastien Tosi; Artur Llobet; Ernest Giralt; Pau Gorostiza
Journal:  Angew Chem Int Ed Engl       Date:  2013-06-17       Impact factor: 15.336

3.  Photochromic blockers of voltage-gated potassium channels.

Authors:  Matthew R Banghart; Alexandre Mourot; Doris L Fortin; Jennifer Z Yao; Richard H Kramer; Dirk Trauner
Journal:  Angew Chem Int Ed Engl       Date:  2009       Impact factor: 15.336

Review 4.  Drugs for allosteric sites on receptors.

Authors:  Cody J Wenthur; Patrick R Gentry; Thomas P Mathews; Craig W Lindsley
Journal:  Annu Rev Pharmacol Toxicol       Date:  2013-10-02       Impact factor: 13.820

Review 5.  Optogenetic pharmacology for control of native neuronal signaling proteins.

Authors:  Richard H Kramer; Alexandre Mourot; Hillel Adesnik
Journal:  Nat Neurosci       Date:  2013-06-25       Impact factor: 24.884

6.  Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.

Authors:  Darren W Engers; Julie R Field; Uyen Le; Ya Zhou; Julie D Bolinger; Rocio Zamorano; Anna L Blobaum; Carrie K Jones; Satyawan Jadhav; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  J Med Chem       Date:  2011-01-19       Impact factor: 7.446

7.  Determinants of metabotropic glutamate receptor-5-mediated Ca2+ and inositol 1,4,5-trisphosphate oscillation frequency. Receptor density versus agonist concentration.

Authors:  Mark S Nash; Michael J Schell; Peter J Atkinson; Neil R Johnston; Stefan R Nahorski; R A John Challiss
Journal:  J Biol Chem       Date:  2002-07-15       Impact factor: 5.157

8.  Photochromic activators of the acetylcholine receptor.

Authors:  E Bartels; N H Wassermann; B F Erlanger
Journal:  Proc Natl Acad Sci U S A       Date:  1971-08       Impact factor: 11.205

Review 9.  Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Arthur Christopoulos; Craig W Lindsley
Journal:  Nat Rev Drug Discov       Date:  2009-01       Impact factor: 84.694

10.  Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery.

Authors:  Arup K Ghose; Torsten Herbertz; Robert L Hudkins; Bruce D Dorsey; John P Mallamo
Journal:  ACS Chem Neurosci       Date:  2011-11-02       Impact factor: 4.418
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  44 in total

Review 1.  Glutamatergic Signaling in the Central Nervous System: Ionotropic and Metabotropic Receptors in Concert.

Authors:  Andreas Reiner; Joshua Levitz
Journal:  Neuron       Date:  2018-06-27       Impact factor: 17.173

Review 2.  Novel Allosteric Modulators of G Protein-coupled Receptors.

Authors:  Patrick R Gentry; Patrick M Sexton; Arthur Christopoulos
Journal:  J Biol Chem       Date:  2015-06-22       Impact factor: 5.157

3.  Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation.

Authors:  Karen J Gregory; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2015-03-25       Impact factor: 4.436

4.  Reversible silencing of endogenous receptors in intact brain tissue using 2-photon pharmacology.

Authors:  Silvia Pittolo; Hyojung Lee; Anna Lladó; Sébastien Tosi; Miquel Bosch; Lídia Bardia; Xavier Gómez-Santacana; Amadeu Llebaria; Eduardo Soriano; Julien Colombelli; Kira E Poskanzer; Gertrudis Perea; Pau Gorostiza
Journal:  Proc Natl Acad Sci U S A       Date:  2019-06-13       Impact factor: 11.205

Review 5.  Synapses in the spotlight with synthetic optogenetics.

Authors:  Shai Berlin; Ehud Y Isacoff
Journal:  EMBO Rep       Date:  2017-04-10       Impact factor: 8.807

6.  Dynamic modulation of inflammatory pain-related affective and sensory symptoms by optical control of amygdala metabotropic glutamate receptor 4.

Authors:  C Zussy; X Gómez-Santacana; X Rovira; D De Bundel; S Ferrazzo; D Bosch; D Asede; F Malhaire; F Acher; J Giraldo; E Valjent; I Ehrlich; F Ferraguti; J-P Pin; A Llebaria; C Goudet
Journal:  Mol Psychiatry       Date:  2016-12-20       Impact factor: 15.992

Review 7.  Optochemical Control of Biological Processes in Cells and Animals.

Authors:  Nicholas Ankenbruck; Taylor Courtney; Yuta Naro; Alexander Deiters
Journal:  Angew Chem Int Ed Engl       Date:  2018-02-01       Impact factor: 15.336

8.  Lighting the way.

Authors: 
Journal:  Nat Chem Biol       Date:  2016-05-18       Impact factor: 15.040

Review 9.  Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders.

Authors:  Daniel J Foster; P Jeffrey Conn
Journal:  Neuron       Date:  2017-05-03       Impact factor: 17.173

Review 10.  Precise modulation of neuronal activity with synthetic photoswitchable ligands.

Authors:  Michael A Kienzler; Ehud Y Isacoff
Journal:  Curr Opin Neurobiol       Date:  2017-07-06       Impact factor: 6.627
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