List of works - Leigh A Stoddart

A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-A3 Receptor in Living Cells

scientific article published on 13 December 2017

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor

scientific article published on 27 March 2019

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

scientific article published on September 2009

Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics

scientific article

Application of BRET to monitor ligand binding to GPCRs

scientific article

Application of Fluorescent Purinoceptor Antagonists for Bioluminescence Resonance Energy Transfer Assays and Fluorescent Microscopy

scientific article published on 01 January 2020

Binding kinetics of ligands acting at GPCRs

scientific article published on 08 February 2019

Class A Orphans (version 2019.5) in the IUPHAR/BPS Guide to Pharmacology Database

Class A Orphans (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database

Class A Orphans in GtoPdb v.2021.3

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

scientific article

Constitutive activity of GPR40/FFA1 intrinsic or assay dependent?

scientific article published on January 2010

Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers.

scientific article published in September 2013

Correction to Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

scientific article published on 24 April 2018

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ)

scientific article published on 27 January 2017

Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells

scientific article

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist.

scientific article published on 30 April 2015

Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization

scientific article published on August 2014

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

scientific article

Fluorescence- and bioluminescence-based approaches to study GPCR ligand binding.

scientific article published on 28 August 2015

Fluorescent ligands for G protein-coupled receptors: illuminating receptor-ligand interactions for drug discovery.

scientific article published in August 2013

Fluorescent ligands: Bringing light to emerging GPCR paradigms

scientific article published on 06 February 2020

Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay

scientific article

Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models

scientific article published on 22 November 2015

Functional homomers and heteromers of dopamine D2L and D3 receptors co-exist at the cell surface

scientific article published on 30 January 2012

G protein-coupled receptors for free fatty acids.

scientific article

Highly potent and selective fluorescent antagonists of the human adenosine A₃ receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold.

scientific article published on 13 February 2012

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

scientific article published on December 2008

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time

scientific article

Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells

scientific article published on 27 November 2020

NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs.

scientific article published on 10 November 2017

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

scientific article published on 6 August 2007

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor.

scientific article published on 27 May 2019

Probing the pharmacology of G protein-coupled receptors with fluorescent ligands.

scientific article published on 13 May 2015

Single molecule binding of a ligand to a G-protein-coupled receptor in real time using fluorescence correlation spectroscopy, rendered possible by nano-encapsulation in styrene maleic acid lipid particles

scientific article published on 19 May 2020

Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor

scientific article published on 09 January 2020

Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

scientific article published on 20 March 2018

Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.

scientific article

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors ⬇️

journal article from 'British Journal of Pharmacology' published in 2021

The Concise Guide to PHARMACOLOGY 2013/14: overview

scientific article

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

scientific article

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

Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells.

scientific article

List of works by Leigh A Stoddart

A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-A3 Receptor in Living Cells

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor

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

Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics

Application of BRET to monitor ligand binding to GPCRs

Application of Fluorescent Purinoceptor Antagonists for Bioluminescence Resonance Energy Transfer Assays and Fluorescent Microscopy

Binding kinetics of ligands acting at GPCRs

Class A Orphans (version 2019.5) in the IUPHAR/BPS Guide to Pharmacology Database

Class A Orphans (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database

Class A Orphans in GtoPdb v.2021.3

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

Constitutive activity of GPR40/FFA1 intrinsic or assay dependent?

Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers.

Correction to Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ)

Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist.

Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization

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

Fluorescence- and bioluminescence-based approaches to study GPCR ligand binding.

Fluorescent ligands for G protein-coupled receptors: illuminating receptor-ligand interactions for drug discovery.

Fluorescent ligands: Bringing light to emerging GPCR paradigms

Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay

Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models

Functional homomers and heteromers of dopamine D2L and D3 receptors co-exist at the cell surface

G protein-coupled receptors for free fatty acids.

Highly potent and selective fluorescent antagonists of the human adenosine A₃ receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold.

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

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time

Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells

NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs.

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

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor.

Probing the pharmacology of G protein-coupled receptors with fluorescent ligands.

Single molecule binding of a ligand to a G-protein-coupled receptor in real time using fluorescence correlation spectroscopy, rendered possible by nano-encapsulation in styrene maleic acid lipid particles

Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor

Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors ⬇️

The Concise Guide to PHARMACOLOGY 2013/14: overview

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

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

Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells.