[HTML][HTML] Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization …
In our previous work, using a fluorescent adenosine-A 3 receptor (A 3 AR) agonist and
fluorescence correlation spectroscopy (FCS), we demonstrated high-affinity labeling of the active …
fluorescence correlation spectroscopy (FCS), we demonstrated high-affinity labeling of the active …
[HTML][HTML] Pharmacology under the microscope: the use of fluorescence correlation spectroscopy to determine the properties of ligand–receptor complexes
SJ Briddon, SJ Hill - Trends in pharmacological sciences, 2007 - cell.com
Recent years have revealed a high degree of structural organisation in the way in which cell-surface
receptors and their associated signalling complexes interact at a molecular level. …
receptors and their associated signalling complexes interact at a molecular level. …
[HTML][HTML] Probing the pharmacology of G protein-coupled receptors with fluorescent ligands
G protein-coupled receptors control a wide range of physiological processes and are the
target for many clinically used drugs. Understanding the way in which receptors bind agonists …
target for many clinically used drugs. Understanding the way in which receptors bind agonists …
Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands
Background and purpose: The introduction of fluorescence‐based techniques, and in
particular the development of fluorescent ligands, has allowed the study of G protein‐coupled …
particular the development of fluorescent ligands, has allowed the study of G protein‐coupled …
[PDF][PDF] Fragment screening at adenosine-A3 receptors in living cells using a fluorescence-based binding assay
LA Stoddart, AJ Vernall, JL Denman, SJ Briddon… - Chemistry & biology, 2012 - cell.com
G protein-coupled receptors (GPCRs) comprise the largest family of transmembrane proteins.
For GPCR drug discovery, it is important that ligand affinity is determined in the correct …
For GPCR drug discovery, it is important that ligand affinity is determined in the correct …
New Fluorescent Adenosine A1-Receptor Agonists That Allow Quantification of Ligand−Receptor Interactions in Microdomains of Single Living Cells
RJ Middleton, SJ Briddon, Y Cordeaux… - Journal of medicinal …, 2007 - ACS Publications
Fluorescence spectroscopy is becoming a valuable addition to the array of techniques available
for scrutinizing ligand−receptor interactions in biological systems. In particular, scanning …
for scrutinizing ligand−receptor interactions in biological systems. In particular, scanning …
[HTML][HTML] Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics
LT May, LJ Bridge, LA Stoddart, SJ Briddon… - The FASEB …, 2011 - ncbi.nlm.nih.gov
A growing awareness indicates that many G-protein-coupled receptors (GPCRs) exist as
homodimers, but the extent of the cooperativity across the dimer interface has been largely …
homodimers, but the extent of the cooperativity across the dimer interface has been largely …
Studying GPCR pharmacology in membrane microdomains: fluorescence correlation spectroscopy comes of age
G protein-coupled receptors (GPCRs) are organised within the cell membrane into highly
ordered macromolecular complexes along with other receptors and signalling proteins. …
ordered macromolecular complexes along with other receptors and signalling proteins. …
Fluorescent ligands: Bringing light to emerging GPCR paradigms
In recent years, several novel aspects of GPCR pharmacology have been described, which
are thought to play a role in determining the in vivo efficacy of a compound. Fluorescent …
are thought to play a role in determining the in vivo efficacy of a compound. Fluorescent …
[HTML][HTML] Single molecule binding of a ligand to a G-protein-coupled receptor in real time using fluorescence correlation spectroscopy, rendered possible by nano …
The fundamental importance of membrane proteins in cellular processes has driven a marked
increase in the use of membrane mimetic approaches for studying and exploiting these …
increase in the use of membrane mimetic approaches for studying and exploiting these …