Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3. (Q37589701)

21 August 2017

1 reference

title

Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3. (English)

1 reference

21 August 2017

0 references

1 reference

2

Leigh A Stoddart

1 reference

21 August 2017

1

Graeme Milligan

1 reference

21 August 2017

Nicola J Smith

3

1 reference

PMCID

2795255

21 August 2017

language of work or name

English

0 references

publication date

1 September 2009

1 reference

British Journal of Pharmacology

21 August 2017

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21 August 2017

158

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21 August 2017

1

1 reference

21 August 2017

146-153

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Sequence polymorphisms provide a common consensus sequence for GPR41 and GPR42

21 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1

23 August 2017

1 reference

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Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B

23 August 2017

1 reference

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

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1, -2, and -3: pharmacology and pathophysiological functions

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81

23 August 2017

1 reference

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Fatty acid binding receptors and their physiological role in type 2 diabetes

23 August 2017

1 reference

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Role of GPR81 in lactate-mediated reduction of adipose lipolysis

23 August 2017

1 reference

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GPR40 carboxylic acid receptor family and diabetes: a new drug target

23 August 2017

1 reference

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Free fatty acid receptors and drug discovery

23 August 2017

1 reference

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Conserved polar residues in transmembrane domains V, VI, and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids

23 August 2017

1 reference

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The long-chain fatty acid receptor, GPR40, and glucolipotoxicity: investigations using GPR40-knockout mice

23 August 2017

1 reference

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

23 August 2017

1 reference

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Seven transmembrane-spanning receptors for free fatty acids as therapeutic targets for diabetes mellitus: pharmacological, phylogenetic, and drug discovery aspects.

23 August 2017

1 reference

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Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening

23 August 2017

1 reference

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Identification of residues important for agonist recognition and activation in GPR40

23 August 2017

1 reference

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

23 August 2017

1 reference

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Medium-chain fatty acids as ligands for orphan G protein-coupled receptor GPR84

23 August 2017

1 reference

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Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox

23 August 2017

1 reference

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Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

G protein-coupled receptors for free fatty acids.

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Short-chain fatty acid receptor, GPR43, is expressed by enteroendocrine cells and mucosal mast cells in rat intestine

23 August 2017

1 reference

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Heterotrimeric G-proteins: a short history

23 August 2017

1 reference

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Techniques: promiscuous Galpha proteins in basic research and drug discovery

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Acetate and propionate short chain fatty acids stimulate adipogenesis via GPCR43

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Citric acid cycle intermediates as ligands for orphan G-protein-coupled receptors

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

The identification of ligands at orphan G-protein coupled receptors

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Short-chain fatty acids stimulate leptin production in adipocytes through the G protein-coupled receptor GPR41

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

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

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

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

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

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

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids

23 August 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1

23 August 2017

1 reference

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Techniques used in the identification and analysis of function of pertussis toxin-sensitive guanine nucleotide binding proteins

23 August 2017

1 reference

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Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes.

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity

14 September 2017

1 reference

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A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

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

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

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

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

(D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G.

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

A novel Galphaq/11-selective inhibitor

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Activation of G protein-coupled receptor 43 in adipocytes leads to inhibition of lipolysis and suppression of plasma free fatty acids

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Identification and characterization of the bovine G protein-coupled receptor GPR41 and GPR43 genes

25 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists

1 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

GPR109A is a G-protein-coupled receptor for the bacterial fermentation product butyrate and functions as a tumor suppressor in colon

1 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.

1 September 2018

1 reference

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Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists

1 September 2018

1 reference

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Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2.

1 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Synthesis and activity of small molecule GPR40 agonists.

1 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2795255

Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction

1 September 2018

1 reference

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Identification of granulocyte subtype-selective receptors and ion channels by using a high-density oligonucleotide probe array.

1 September 2018

1 reference

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A chemogenomic analysis of the transmembrane binding cavity of human G-protein-coupled receptors

1 September 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/19719777

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Orphan seven transmembrane receptor screening

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/19719777

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Activation of MAPKs by G protein-coupled receptors

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/19719777

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1111/J.1476-5381.2009.00421.X

1 reference

21 August 2017

1 reference

21 August 2017

1 reference

PMCID

2795255