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Complex Pharmacology of Free Fatty Acid Receptors

Chemical reviews, 2017-01, Vol.117 (1), p.67-110

2017

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Discovery of a Potent and Selective GPR120 Agonist

Journal of medicinal chemistry, 2012-05, Vol.55 (9), p.4511-4515

2012

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The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism

Molecular pharmacology, 2013-11, Vol.84 (5), p.710-725

2013

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The Molecular Basis of Ligand Interaction at Free Fatty Acid Receptor 4 (FFA4/GPR120)

The Journal of biological chemistry, 2014-07, Vol.289 (29), p.20345-20358

2014

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Metabolite-sensing GPCRs controlling interactions between adipose tissue and inflammation

Frontiers in endocrinology (Lausanne), 2023-07, Vol.14, p.1197102-1197102

2023

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Extracellular Ionic Locks Determine Variation in Constitutive Activity and Ligand Potency between Species Orthologs of the Free Fatty Acid Receptors FFA2 and FFA3

The Journal of biological chemistry, 2012-11, Vol.287 (49), p.41195-41209

2012

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Chemogenetics defines receptor-mediated functions of short chain free fatty acids

Nature chemical biology, 2019-05, Vol.15 (5), p.489-498

2019

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Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4849-4858

2016

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Treatment of type 2 diabetes by free Fatty Acid receptor agonists

Frontiers in endocrinology (Lausanne), 2014-01, Vol.5, p.137-137

2014

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Distinct Phosphorylation Clusters Determine the Signaling Outcome of Free Fatty Acid Receptor 4/G Protein-Coupled Receptor 120

Molecular pharmacology, 2016-05, Vol.89 (5), p.505-520

2016

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Defining the Molecular Basis for the First Potent and Selective Orthosteric Agonists of the FFA2 Free Fatty Acid Receptor

The Journal of biological chemistry, 2013-06, Vol.288 (24), p.17296-17312

2013

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Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)

Journal of medicinal chemistry, 2017-07, Vol.60 (13), p.5638-5645

2017

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The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs

Current topics in medicinal chemistry, 2013-01, Vol.13 (1), p.14-25

2013

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Chemogenetics defines a short-chain fatty acid receptor gut-brain axis

eLife, 2022-03, Vol.11

2022

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Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of Agonist Versus Antagonist Ligands

The Journal of biological chemistry, 2016-01, Vol.291 (1), p.303-317

2016

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A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor

Cell chemical biology, 2016-03, Vol.23 (3), p.392-403

2016

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Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands

Molecular pharmacology, 2014-08, Vol.86 (2), p.200-210

2014

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Minireview: The Effects of Species Ortholog and SNP Variation on Receptors for Free Fatty Acids

Molecular endocrinology (Baltimore, Md.), 2013-08, Vol.27 (8), p.1177-1187

2013

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Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs

The FASEB journal, 2012-12, Vol.26 (12), p.4951-4965

2012

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Mechanism and function of Drosophila capa GPCR: a desiccation stress-responsive receptor with functional homology to human neuromedinU receptor

PloS one, 2012-01, Vol.7 (1), p.e29897-e29897

2012

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Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4

Molecular pharmacology, 2017-06, Vol.91 (6), p.630-641

2017

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Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13

Biochemical journal, 2010-12, Vol.432 (3), p.451-459

2010

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The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35

Molecular pharmacology, 2014-01, Vol.85 (1), p.91-104

2014

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A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias

Scientific reports, 2017-10, Vol.7 (1), p.13741-15, Article 13741

2017

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Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine‐to‐isoleucine variation

The FASEB journal, 2019-04, Vol.33 (4), p.5005-5017

2019

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Complex Pharmacology of Free Fatty Acid Receptors

Discovery of a Potent and Selective GPR120 Agonist

The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism

The Molecular Basis of Ligand Interaction at Free Fatty Acid Receptor 4 (FFA4/GPR120)

Metabolite-sensing GPCRs controlling interactions between adipose tissue and inflammation

Extracellular Ionic Locks Determine Variation in Constitutive Activity and Ligand Potency between Species Orthologs of the Free Fatty Acid Receptors FFA2 and FFA3

Chemogenetics defines receptor-mediated functions of short chain free fatty acids

Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer

Treatment of type 2 diabetes by free Fatty Acid receptor agonists

Distinct Phosphorylation Clusters Determine the Signaling Outcome of Free Fatty Acid Receptor 4/G Protein-Coupled Receptor 120

Defining the Molecular Basis for the First Potent and Selective Orthosteric Agonists of the FFA2 Free Fatty Acid Receptor

Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)

The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs

Chemogenetics defines a short-chain fatty acid receptor gut-brain axis

Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of Agonist Versus Antagonist Ligands

A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor

Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands

Minireview: The Effects of Species Ortholog and SNP Variation on Receptors for Free Fatty Acids

Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs

Mechanism and function of Drosophila capa GPCR: a desiccation stress-responsive receptor with functional homology to human neuromedinU receptor

Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4

Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13

The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35

A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias

Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine‐to‐isoleucine variation

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