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

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Huixian Wu

Huixian Wu

1

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Karen J. Gregory

Karen J Gregory

3

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Jens Meiler

Jens Meiler

9

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Raymond C. Stevens

Raymond C Stevens

12

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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

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

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

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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

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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

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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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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.

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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

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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

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

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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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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

1 reference

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

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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

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

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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

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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

1 reference

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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

1762007

ADS bibcode

2014Sci...344...58W

0 references

1762007

1 reference

1 reference

1 reference