GPR40 agonists for the treatment of type 2 diabetes: life after 'TAKing' a hit. (Q38325894)

2 September 2017

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title

GPR40 agonists for the treatment of type 2 diabetes: life after 'TAKing' a hit. (English)

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2 September 2017

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2

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25604916%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

author name string

A D Mancini

series ordinal

1

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25604916%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

publication date

24 February 2015

1 reference

Diabetes, Obesity and Metabolism

2 September 2017

published in

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25604916%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

volume

17

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25604916%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

issue

7

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25604916%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

page(s)

622-629

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25604916%20AND%20SRC:MED&resulttype=core&format=json

Circulating fatty acids are essential for efficient glucose-stimulated insulin secretion after prolonged fasting in humans

31 May 2020

cites work

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Essentiality of circulating fatty acids for glucose-stimulated insulin secretion in the fasted rat.

21 January 2018

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Stimulation of insulin secretion by infusion of free fatty acids

21 January 2018

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

21 January 2018

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

21 January 2018

1 reference

Progress in methodology. Improved reporter gene assays used to identify ligands acting on orphan seven-transmembrane receptors

21 January 2018

1 reference

Metabolic signaling in fuel-induced insulin secretion

21 January 2018

1 reference

The Gq/G11-mediated signaling pathway is critical for autocrine potentiation of insulin secretion in mice

21 January 2018

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G protein-coupled receptor (GPR)40-dependent potentiation of insulin secretion in mouse islets is mediated by protein kinase D1.

21 January 2018

1 reference

Mechanisms of biphasic insulin-granule exocytosis - roles of the cytoskeleton, small GTPases and SNARE proteins

21 January 2018

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

21 January 2018

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Deletion of GPR40 impairs glucose-induced insulin secretion in vivo in mice without affecting intracellular fuel metabolism in islets

21 January 2018

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Increased glucose metabolism and glycerolipid formation by fatty acids and GPR40 receptor signaling underlies the fatty acid potentiation of insulin secretion

21 January 2018

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

21 January 2018

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Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from beta-cells through activation of GPR40.

21 January 2018

1 reference

Free fatty acid receptor 1 (FFA(1)R/GPR40) and its involvement in fatty-acid-stimulated insulin secretion.

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

The fatty acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding.

21 January 2018

1 reference

Lack of FFAR1/GPR40 does not protect mice from high-fat diet-induced metabolic disease

21 January 2018

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Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice

21 January 2018

1 reference

Glucolipotoxicity of the pancreatic beta cell.

21 January 2018

1 reference

FFAR1 is involved in both the acute and chronic effects of palmitate on insulin secretion

21 January 2018

1 reference

DC260126: a small-molecule antagonist of GPR40 that protects against pancreatic β-Cells dysfunction in db/db mice

21 January 2018

1 reference

DC260126, a small-molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats

21 January 2018

1 reference

Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice

21 January 2018

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GPR40 is partially required for insulin secretion following activation of beta3-adrenergic receptors

21 January 2018

1 reference

AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents

21 January 2018

1 reference

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

21 January 2018

1 reference

TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats

21 January 2018

1 reference

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

21 January 2018

1 reference

GPR40: good cop, bad cop?

21 January 2018

1 reference

Glucolipotoxicity age-dependently impairs beta cell function in rats despite a marked increase in beta cell mass

21 January 2018

1 reference

Expression of the gene for a membrane-bound fatty acid receptor in the pancreas and islet cell tumours in humans: evidence for GPR40 expression in pancreatic beta cells and implications for insulin secretion

21 January 2018

1 reference

G-protein-coupled receptor 40 (GPR40) expression and its regulation in human pancreatic islets: the role of type 2 diabetes and fatty acids

21 January 2018

1 reference

CNX-011-67, a novel GPR40 agonist, enhances glucose responsiveness, insulin secretion and islet insulin content in n-STZ rats and in islets from type 2 diabetic patients.

21 January 2018

1 reference

Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes

21 January 2018

1 reference

Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist

21 January 2018

1 reference

Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet beta-cells: mediation by PLC and L-type Ca2+ channel and link to insulin release

21 January 2018

1 reference

Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway.

21 January 2018

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Reduction in voltage-gated K+ currents in primary cultured rat pancreatic beta-cells by linoleic acids

21 January 2018

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Signaling mechanisms of glucose-induced F-actin remodeling in pancreatic islet β cells

21 January 2018

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

21 January 2018

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Therapeutic potential of β-arrestin- and G protein-biased agonists.

21 January 2018

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Recent developments in biased agonism

21 January 2018

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

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

21 January 2018

1 reference

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

21 January 2018

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Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells.

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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Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition

21 January 2018

1 reference

The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets.

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Treatment with CNX-011-67, a novel GPR40 agonist, delays onset and progression of diabetes and improves beta cell preservation and function in male ZDF rats

21 January 2018

1 reference

Bridging the gap: bitopic ligands of G-protein-coupled receptors.

21 January 2018

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

21 January 2018

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

21 January 2018

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

21 January 2018

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles

21 January 2018

1 reference

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

21 January 2018

1 reference

Acute stimulation of glucagon secretion by linoleic acid results from GPR40 activation and [Ca2+]i increase in pancreatic islet {alpha}-cells

21 January 2018

1 reference

Regulation of the gene encoding GPR40, a fatty acid receptor expressed selectively in pancreatic beta cells

21 January 2018

1 reference

Expression of free fatty acid receptor GPR40 in the neurogenic niche of adult monkey hippocampus

21 January 2018

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Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system

21 January 2018

1 reference

Hypothalamic GPR40 signaling activated by free long chain fatty acids suppresses CFA-induced inflammatory chronic pain

21 January 2018

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New insights into "GPR40-CREB interaction in adult neurogenesis" specific for primates.

21 January 2018

1 reference

Taste Preference for Fatty Acids Is Mediated by GPR40 and GPR120

21 January 2018

1 reference

Fatty acid receptor Gpr40 mediates neuromicrovascular degeneration induced by transarachidonic acids in rodents

21 January 2018

1 reference

Optimization of GPR40 Agonists for Type 2 Diabetes.

21 January 2018

1 reference

Modulation of osteoclastogenesis by fatty acids

21 January 2018

1 reference

Thiazolidinediones induce osteocyte apoptosis by a G protein-coupled receptor 40-dependent mechanism.

21 January 2018

1 reference

The free fatty acid receptor G protein-coupled receptor 40 (GPR40) protects from bone loss through inhibition of osteoclast differentiation.

21 January 2018

1 reference

GLP-1 receptor agonists for individualized treatment of type 2 diabetes mellitus

21 January 2018

1 reference

21 January 2018

Identifiers

DOI

10.1111/DOM.12442

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:25604916%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

1 reference