Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator (Q24338769)

positive regulation of cytosolic calcium ion concentration involved in phospholipase C-activating G protein-coupled signaling pathway

GOA release 2020-03-11

1 reference

GOA release 2020-03-11

author

Vsevolod Katritch

8

0 references

Vadim Cherezov

10

0 references

Huixian Wu

Huixian Wu

1

0 references

Karen J. Gregory

Karen J Gregory

3

0 references

Jens Meiler

Jens Meiler

9

0 references

Raymond C. Stevens

Raymond C Stevens

12

0 references

Colleen M. Niswender

7

Colleen M Niswender

0 references

P. Jeffrey Conn

11

P Jeffrey Conn

0 references

Hyekyung P Cho

5

Hyekyung P Cho

0 references

Gye Won Han

4

Gye Won Han

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author name string

Chong Wang

2

0 references

Yan Xia

Structure of class B GPCR corticotropin-releasing factor receptor 1

6

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language of work or name

English

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publication date

4 April 2014

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published in

Science

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volume

344

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issue

6179

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page(s)

58-64

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cites work

1 reference

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22 April 2017

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Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site

22 April 2017

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Structural diversity of G protein-coupled receptors and significance for drug discovery

22 April 2017

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Crystallizing membrane proteins using lipidic mesophases

7 April 2017

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Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors

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Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology

27 September 2017

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Structure-function of the G protein-coupled receptor superfamily

27 September 2017

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Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

27 September 2017

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Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships

27 September 2017

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Interdomain movements in metabotropic glutamate receptor activation

27 September 2017

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Dimers and beyond: The functional puzzles of class C GPCRs.

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27 September 2017

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N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors

27 September 2017

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Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTID

27 September 2017

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Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP.

27 September 2017

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Glutamate-binding affinity of Drosophila metabotropic glutamate receptor is modulated by association with lipid rafts.

27 September 2017

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Mutational Analysis and Molecular Modeling of the Binding Pocket of the Metabotropic Glutamate 5 Receptor Negative Modulator 2-Methyl-6-(phenylethynyl)-pyridine

27 September 2017

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Cloning, expression, and gene structure of a G protein-coupled glutamate receptor from rat brain

30 May 2018

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Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist

30 May 2018

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Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one

21 January 2018

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ROSETTALIGAND: protein-small molecule docking with full side-chain flexibility.

21 January 2018

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Fusion partner toolchest for the stabilization and crystallization of G protein-coupled receptors

21 January 2018

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Development of an Automated High Throughput LCP-FRAP Assay to Guide Membrane Protein Crystallization in Lipid Mesophases

21 January 2018

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Rastering strategy for screening and centring of microcrystal samples of human membrane proteins with a sub-10 microm size X-ray synchrotron beam.

21 January 2018

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Processing of X-ray diffraction data collected in oscillation mode

21 January 2018

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A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling

21 January 2018

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A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators

21 January 2018

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JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist

21 January 2018

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Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.

21 January 2018

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Switch in the expression of mGlu1 and mGlu5 metabotropic glutamate receptors in the cerebellum of mice developing experimental autoimmune encephalomyelitis and in autoptic cerebellar samples from patients with multiple sclerosis.

21 January 2018

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Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1.

21 January 2018

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Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers

21 January 2018

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Assessment and challenges of ligand docking into comparative models of G-protein coupled receptors

21 January 2018

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[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.

21 January 2018

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Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors.

21 January 2018

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Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors

21 January 2018

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Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolin

21 January 2018

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Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators

21 January 2018

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Transposition of three amino acids transforms the human metabotropic glutamate receptor (mGluR)-3-positive allosteric modulation site to mGluR2, and additional characterization of the mGluR2-positive allosteric modulation site

21 January 2018

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Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2.

21 January 2018

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Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators

21 January 2018

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Homology modeling of the transmembrane domain of the human calcium sensing receptor and localization of an allosteric binding site

21 January 2018

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Positive and negative allosteric modulators of the Ca2+-sensing receptor interact within overlapping but not identical binding sites in the transmembrane domain

21 January 2018

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Modeling and Mutagenesis of the Binding Site of Calhex 231, a Novel Negative Allosteric Modulator of the Extracellular Ca2+-sensing Receptor

21 January 2018

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Point mutations in the transmembrane region of GABAB2 facilitate activation by the positive modulator N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the absence of the GABAB1 subunit.

21 January 2018

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The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate recepto

21 January 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24603153

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1126/SCIENCE.1249489

1 reference

ADS bibcode

2014Sci...344...58W

0 references

1 reference

1 reference

PubMed publication ID

24603153

1 reference