GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo (Q35040481)

6 August 2017

title

GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo (English)

1 reference

6 August 2017

Maria Hauge

1

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Anna Sofie Husted

Anna S Husted

3

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Michael Lückmann

Michael Lückmann

10

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Jeppe Pio Ekberg

Jeppe P Ekberg

4

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Birgitte Holst

Birgitte Holst

14

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Thue W Schwartz

Thue W Schwartz

16

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Michael W. Miller

11

Michael W Miller

1 reference

6 August 2017

Marie A Vestmar

2

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6 August 2017

Michael J Wright

5

1 reference

6 August 2017

Jerry Di Salvo

6

1 reference

6 August 2017

Adam B Weinglass

7

1 reference

6 August 2017

Maja S Engelstoft

8

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6 August 2017

Andreas N Madsen

9

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6 August 2017

Maria E Trujillo

12

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6 August 2017

Thomas M Frimurer

13

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6 August 2017

Andrew D Howard

15

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6 August 2017

publication date

24 October 2014

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6 August 2017

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6 August 2017

volume

4

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6 August 2017

issue

1

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6 August 2017

page(s)

3-14

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

6 August 2017

cites work

1 reference

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8 July 2018

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Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles

8 July 2018

1 reference

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Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist

8 July 2018

1 reference

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

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

Recent developments in biased agonism

8 July 2018

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Expression of the fatty acid receptor GPR120 in the gut of diet-induced-obese rats and its role in GLP-1 secretion

8 July 2018

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Enteroendocrine cell types revisited

8 July 2018

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

8 July 2018

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Enteroendocrine hormone mimetics for the treatment of obesity and diabetes

8 July 2018

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Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes

8 July 2018

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The fatty acid receptor FFA1/GPR40 a decade later: how much do we know?

8 July 2018

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Activation of FFA1 mediates GLP-1 secretion in mice. Evidence for allosterism at FFA1.

8 July 2018

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Reevaluation of fatty acid receptor 1 as a drug target for the stimulation of insulin secretion in humans

8 July 2018

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8 July 2018

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A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents

8 July 2018

1 reference

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

8 July 2018

1 reference

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Docking and scoring with ICM: the benchmarking results and strategies for improvement

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

8 July 2018

GPR119 as a fat sensor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

G-protein-coupled receptors in intestinal chemosensation

8 July 2018

1 reference

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Axon-like basal processes in enteroendocrine cells: characteristics and potential targets

8 July 2018

1 reference

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Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

The G-protein-coupled receptor GPR40 directly mediates long-chain fatty acid-induced secretion of cholecystokinin

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

Epac: defining a new mechanism for cAMP action

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

GPR119 agonists for the treatment of type 2 diabetes

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

Ligand binding and micro-switches in 7TM receptor structures

8 July 2018

1 reference

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Discovery of new GPCR biology: one receptor structure at a time

8 July 2018

1 reference

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Nutrient-dependent secretion of glucose-dependent insulinotropic polypeptide from primary murine K cells

8 July 2018

1 reference

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Glucose sensing in L cells: a primary cell study

8 July 2018

1 reference

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Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion

8 July 2018

1 reference

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New G-protein-coupled receptor crystal structures: insights and limitations

8 July 2018

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The Physiology of Glucagon-like Peptide 1

8 July 2018

1 reference

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Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act?

8 July 2018

1 reference

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GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo.

8 July 2018

1 reference

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Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules

8 July 2018

1 reference

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Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents

8 July 2018

1 reference

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PKA-dependent and PKA-independent pathways for cAMP-regulated exocytosis

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

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

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

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

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

G protein-coupled receptor allosterism and complexing

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

Is there a 'lock' for all agonist 'keys' in 7TM receptors?

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

A multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel GPR40 agonist, TAK-875, in subjects with type 2 diabetes

8 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

A gut feeling for obesity: 7TM sensors on enteroendocrine cells

25 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse

25 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

Glucagon-like peptide-1 (7-36)amide and glucose-dependent insulinotropic polypeptide secretion in response to nutrient ingestion in man: acute post-prandial and 24-h secretion patterns.

25 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4314522

Effects of PYY3–36 and GLP-1 on energy intake, energy expenditure, and appetite in overweight men

25 October 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/25685685

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/25685685

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1016/J.MOLMET.2014.10.002

1 reference

6 August 2017

1 reference

6 August 2017

1 reference