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NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs

Trends in pharmacological sciences (Regular ed.), 2018-02, Vol.39 (2), p.136-147

2018

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

Pharmacological reviews, 2008-12, Vol.60 (4), p.405

2008

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Application of BRET to monitor ligand binding to GPCRs

Nature methods, 2015-07, Vol.12 (7), p.661

2015

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Fluorescence‐ and bioluminescence‐based approaches to study GPCR ligand binding

British journal of pharmacology, 2016-10, Vol.173 (20), p.3028-3037

2016

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

Drug discovery today, 2017-06, Vol.22 (6), p.896-911

2017

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

Scientific reports, 2018-01, Vol.8 (1), p.1-19, Article 1572

2018

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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

The Journal of biological chemistry, 2008-11, Vol.283 (47), p.32913-32924

2008

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The Action and Mode of Binding of Thiazolidinedione Ligands at Free Fatty Acid Receptor 1

The Journal of biological chemistry, 2009-06, Vol.284 (26), p.17527-17539

2009

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

British journal of pharmacology, 2009-09, Vol.158 (1), p.146-153

2009

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

Molecular pharmacology, 2011-07, Vol.80 (1), p.163-173

2011

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

Frontiers in pharmacology, 2017-12, Vol.8, p.908-908

2017

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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

Molecular pharmacology, 2007-04, Vol.71 (4), p.994-1005

2007

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Fluorescent ligands: Bringing light to emerging GPCR paradigms

British journal of pharmacology, 2020-03, Vol.177 (5), p.978-991

2020

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Binding kinetics of ligands acting at GPCRs

Molecular and cellular endocrinology, 2019-04, Vol.485, p.9-19

2019

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Advances in the application of fluorescence correlation spectroscopy to study detergent purified and encapsulated membrane proteins

The international journal of biochemistry & cell biology, 2022-05, Vol.146, p.106210-106210, Article 106210

2022

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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

Pharmacology research & perspectives, 2016-10, Vol.4 (5), p.e00250-n/a

2016

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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

Nanoscale, 2020-06, Vol.12 (21), p.11518-11525

2020

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

Neuropharmacology, 2015-11, Vol.98, p.48-57

2015

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

Journal of medicinal chemistry, 2015-12, Vol.58 (24), p.9578-9590

2015

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

Journal of medicinal chemistry, 2020-03, Vol.63 (5), p.2656-2672

2020

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Efficient G protein coupling is not required for agonist‐mediated internalization and membrane reorganization of the adenosine A3 receptor

The FASEB journal, 2021-04, Vol.35 (4), p.e21211-n/a

2021

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Efficient G protein coupling is not required for agonist-mediated internalization and membrane reorganization of the adenosine A 3 receptor

The FASEB journal, 2021-04, Vol.35 (4), p.e21211

2021

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Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor

Journal of medicinal chemistry, 2023-04, Vol.66 (7), p.5208-5222

2023

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Detection of genome‐edited and endogenously expressed G protein‐coupled receptors

The FEBS journal, 2021-04, Vol.288 (8), p.2585-2601

2021

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Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H 1 Receptor

Journal of medicinal chemistry, 2022-06, Vol.65 (12), p.8258-8288

2022

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NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs

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

Application of BRET to monitor ligand binding to GPCRs

Fluorescence‐ and bioluminescence‐based approaches to study GPCR ligand binding

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

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

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

The Action and Mode of Binding of Thiazolidinedione Ligands at Free Fatty Acid Receptor 1

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

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

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

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

Fluorescent ligands: Bringing light to emerging GPCR paradigms

Binding kinetics of ligands acting at GPCRs

Advances in the application of fluorescence correlation spectroscopy to study detergent purified and encapsulated membrane proteins

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

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

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

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

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

Efficient G protein coupling is not required for agonist‐mediated internalization and membrane reorganization of the adenosine A3 receptor

Efficient G protein coupling is not required for agonist-mediated internalization and membrane reorganization of the adenosine A 3 receptor

Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor

Detection of genome‐edited and endogenously expressed G protein‐coupled receptors

Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H 1 Receptor

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