High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875 (Q24301044)

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10 March 2020

title

High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875 (English)

1 reference

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Free fatty acid receptor 1

10 March 2020

main subject

1 reference

GOA release 2020-03-11

author

Franz Gruswitz

5

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10 March 2020

author name string

Ankita Srivastava

1

1 reference

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10 March 2020

Jason Yano

2

1 reference

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10 March 2020

Yoshihiko Hirozane

3

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10 March 2020

Georgia Kefala

4

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10 March 2020

Gyorgy Snell

6

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10 March 2020

Weston Lane

7

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10 March 2020

Anthony Ivetac

8

1 reference

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10 March 2020

Kathleen Aertgeerts

9

1 reference

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10 March 2020

Jasmine Nguyen

10

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10 March 2020

Andy Jennings

11

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10 March 2020

Kengo Okada

12

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10 March 2020

language of work or name

English

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publication date

20 July 2014

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10 March 2020

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10 March 2020

volume

513

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10 March 2020

issue

7516

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10 March 2020

page(s)

124-127

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Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.

10 March 2020

cites work

1 reference

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Fatty acids, lipotoxicity and insulin secretion

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist

21 January 2018

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Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor

21 January 2018

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GPR40 is expressed in glucagon producing cells and affects glucagon secretion.

21 January 2018

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A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs

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Role of GPR40 in fatty acid action on the beta cell line INS-1E.

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Structure of the agonist-bound neurotensin receptor

21 January 2018

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Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

21 January 2018

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Crystal structure of a lipid G protein-coupled receptor

21 January 2018

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Structure of the δ-opioid receptor bound to naltrindole

21 January 2018

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High-resolution crystal structure of human protease-activated receptor 1

21 January 2018

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Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists

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Structure of the human κ-opioid receptor in complex with JDTic

21 January 2018

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A ligand channel through the G protein coupled receptor opsin

21 January 2018

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hCB2 ligand-interaction landscape: cysteine residues critical to biarylpyrazole antagonist binding motif and receptor modulation

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A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor

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Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.

21 January 2018

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Identification of residues important for agonist recognition and activation in GPR40

21 January 2018

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Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation.

21 January 2018

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Activation and allosteric modulation of a muscarinic acetylcholine receptor

21 January 2018

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Structure-function of the G protein-coupled receptor superfamily

21 January 2018

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Crystal structure of the β2 adrenergic receptor-Gs protein complex

21 January 2018

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Structure of a nanobody-stabilized active state of the β(2) adrenoceptor

21 January 2018

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Crystal Structure of a Thermally Stable Rhodopsin Mutant

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Transmembrane signaling by GPCRs: insight from rhodopsin and opsin structures.

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GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function

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Crystallizing membrane proteins using lipidic mesophases

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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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Mini-beam collimator enables microcrystallography experiments on standard beamlines

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Processing of X-ray diffraction data collected in oscillation mode

21 January 2018

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Scaling and assessment of data quality

21 January 2018

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Presenting your structures: the CCP4mg molecular-graphics software

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A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1

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12 December 2020

Generating thermostabilized agonist-bound GPR40/FFAR1 using virus-like particles and a label-free binding assay

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Identifiers

DOI

10.1038/NATURE13494

2 references

Consolidated OpenCitations Corpus – April 2017

759978

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25043059%20AND%20SRC:MED&resulttype=core&format=json

Dimensions Publication ID

10 March 2020

1047218848

0 references

759978

1 reference

Consolidated OpenCitations Corpus – April 2017

Consolidated OpenCitations Corpus – April 2017

2 references

759978