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List of works by Graeme Milligan

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

scientific article

A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias

scientific article published on 05 July 2016

A general method to quantify ligand-driven oligomerization from fluorescence-based images

scientific article published on 20 May 2019

A single amino acid determines preference between phospholipids and reveals length restriction for activation of the S1P4 receptor

scientific article published on 6 August 2004

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

scientific article

Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases

scientific article published on 28 April 2015

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

scientific article published on September 2009

Allostery at G Protein-Coupled Receptor Homo- and Heteromers: Uncharted Pharmacological Landscapes ⬇️

scientific article published on December 1, 2010

Author Correction: Combinatorial expression of GPCR isoforms affects signalling and drug responses

scientific article published on 25 November 2020

Beta-arrestin 2-dependent angiotensin II type 1A receptor-mediated pathway of chemotaxis

scientific article

Building a new conceptual framework for receptor heteromers

scientific article

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

scientific article published on 23 August 2012

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

scientific article published on 15 April 2019

Chemokine receptor CXCR4 oligomerization is disrupted selectively by the antagonist ligand IT1t

scientific article published on 01 December 2020

Combinatorial expression of GPCR isoforms affects signalling and drug responses

scientific article published on 04 November 2020

Complex Pharmacology of Free Fatty Acid Receptors.

scientific article published on 14 June 2016

Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands

scientific article

Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4

scientific article published on 9 May 2014

Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor

scientific article

Design, Synthesis, and Evaluation of a Diazirine Photoaffinity Probe for Ligand-Based Receptor Capture Targeting G Protein-Coupled Receptors

scientific article published on 04 December 2018

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

scientific article

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

scientific article published on 13 April 2016

Dietary fibers inhibit obesity in mice, but host responses in the cecum and liver appear unrelated to fiber-specific changes in cecal bacterial taxonomic composition

scientific article published in Scientific Reports

Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy.

scientific article published on March 2016

Discovery of a potent and selective GPR120 agonist.

scientific article published on 2 May 2012

Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability.

scientific article published on 22 January 2013

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

scientific article published on 12 February 2016

Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-selective Antagonist Drugs.

scientific article

Evidence for the Existence of a CXCL17 Receptor Distinct from GPR35.

scientific article published on 6 June 2018

Experimental challenges to targeting poorly characterized GPCRs: uncovering the therapeutic potential for free fatty acid receptors.

scientific article published on January 2011

Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3.

scientific article published on 12 October 2012

Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator

scientific article

FFA4/GPR120: Pharmacology and Therapeutic Opportunities.

scientific article

Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance

scientific article

Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties

scientific article published on 13 July 2012

G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35.

scientific article

G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor

scientific article

G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets

scientific article published on 2 January 2014

GPCR-OKB: the G Protein Coupled Receptor Oligomer Knowledge Base.

scientific article

High-content assays for ligand regulation of G-protein-coupled receptors

scientific article (publication date: July 2003)

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

scientific article

Indomethacin treatment prevents high fat diet-induced obesity and insulin resistance but not glucose intolerance in C57BL/6J mice

scientific article

International Union of Basic and Clinical Pharmacology. LXVII. Recommendations for the recognition and nomenclature of G protein-coupled receptor heteromultimers.

scientific article published on March 2007

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

scientific article published on December 2008

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

scientific article (publication date: 2012)

Metabolism meets immunity: The role of free fatty acid receptors in the immune system

scientific article

Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids.

scientific article published on 17 May 2013

Morphine desensitization, internalization, and down-regulation of the mu opioid receptor is facilitated by serotonin 5-hydroxytryptamine2A receptor coactivation

scientific article

Muscarinic receptor oligomerization.

scientific article published on 13 November 2017

Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity

scientific article published on 29 August 2016

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

scientific article published on 29 October 2015

Novel pharmacological applications of G-protein-coupled receptor-G protein fusions

scientific article published on 6 August 2007

On-target and off-target effects of novel orthosteric and allosteric activators of GPR84

scientific article published in Scientific Reports

Palmitoylation regulates regulator of G-protein signaling (RGS) 16 function. II. Palmitoylation of a cysteine residue in the RGS box is critical for RGS16 GTPase accelerating activity and regulation of Gi-coupled signalling

scientific article (publication date: 23 May 2003)

Palmitoylation regulates regulators of G-protein signaling (RGS) 16 function. I. Mutation of amino-terminal cysteine residues on RGS16 prevents its targeting to lipid rafts and palmitoylation of an internal cysteine residue

scientific article (publication date: 23 May 2003)

Pathophysiological regulation of lung function by the free fatty acid receptor FFA4

scientific article published on 01 August 2020

Presynaptic control of striatal glutamatergic neurotransmission by adenosine A1-A2A receptor heteromers

scientific article

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

scientific article

Selective interactions between helix VIII of the human mu-opioid receptors and the C terminus of periplakin disrupt G protein activation

scientific article (publication date: 29 August 2003)

Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3

scientific article

Src-mediated RGS16 tyrosine phosphorylation promotes RGS16 stability

scientific article (publication date: 2 May 2003)

Structural and biophysical characterisation of G protein-coupled receptor ligand binding using resonance energy transfer and fluorescent labelling techniques ⬇️

scientific article published on April 13, 2013

Targeted Elimination of G Proteins and Arrestins Defines Their Specific Contributions to Both Intensity and Duration of G Protein-coupled Receptor Signaling.

scientific article published on 16 November 2016

The First 50 Years of Molecular Pharmacology

scientific article

The M<sub>1</sub> muscarinic receptor is present in situ as a ligand-regulated mixture of monomers and oligomeric complexes

scientific article published on 07 June 2022

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

scientific article published on 10 October 2013

The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120).

scientific article published on 24 May 2014

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

scientific article published on 26 August 2013

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

scientific article published on January 2013

Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84

scientific article published on 01 September 2020

Treatment of type 2 diabetes by free Fatty Acid receptor agonists

scientific article published on 28 August 2014

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

scientific article

Up-regulation of the angiotensin II type 1 receptor by the MAS proto-oncogene is due to constitutive activation of Gq/G11 by MAS

scientific article

beta-Arrestin 1 and Galphaq/11 coordinately activate RhoA and stress fiber formation following receptor stimulation

scientific article

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