Extracellular purines, purinergic receptors and tumor growth

F Di Virgilio, E Adinolfi - Oncogene, 2017 - nature.com
Virtually, all tumor cells as well as all immune cells express plasma membrane receptors for
extracellular nucleosides (adenosine) and nucleotides (ATP, ADP, UTP, UDP and sugar …

Basic pharmacological and structural evidence for class A G-protein-coupled receptor heteromerization

R Franco, E Martínez-Pinilla, JL Lanciego… - Frontiers in …, 2016 - frontiersin.org
Cell membrane receptors rarely work on isolation, often they form oligomeric complexes with
other receptor molecules and they may directly interact with different proteins of the signal …

G protein-coupled receptor-G protein interactions: a single-molecule perspective

D Calebiro, Z Koszegi, Y Lanoiselée… - Physiological …, 2021 - journals.physiology.org
G protein-coupled receptors (GPCRs) regulate many cellular and physiological processes,
responding to a diverse range of extracellular stimuli including hormones, neurotransmitters …

Labeling and single-molecule methods to monitor G protein-coupled receptor dynamics

H Tian, A Furstenberg, T Huber - Chemical reviews, 2017 - ACS Publications
The superfamily of G protein-coupled receptors (GPCRs) mediates a wide range of
physiological responses and serves as an important category of drug targets. Earlier …

NanoBRET approaches to study ligand binding to GPCRs and RTKs

LA Stoddart, LE Kilpatrick, SJ Hill - Trends in pharmacological sciences, 2018 - cell.com
Recent advances in the development of fluorescent ligands for G-protein-coupled receptors
(GPCRs) and receptor tyrosine kinase receptors (RTKs) have facilitated the study of these …

Protein–ligand (un) binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling

M Bernetti, A Cavalli, L Mollica - MedChemComm, 2017 - pubs.rsc.org
In the last three decades, protein and nucleic acid structure determination and
comprehension of the mechanisms, leading to their physiological and pathological …

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

LA Stoddart, LE Kilpatrick, SJ Briddon, SJ Hill - Neuropharmacology, 2015 - Elsevier
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 …

Single molecule binding of a ligand to a G-protein-coupled receptor in real time using fluorescence correlation spectroscopy, rendered possible by nano …

RL Grime, J Goulding, R Uddin, LA Stoddart, SJ Hill… - Nanoscale, 2020 - pubs.rsc.org
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 …

Studying GPCR pharmacology in membrane microdomains: fluorescence correlation spectroscopy comes of age

SJ Briddon, LE Kilpatrick, SJ Hill - Trends in pharmacological sciences, 2018 - cell.com
G protein-coupled receptors (GPCRs) are organised within the cell membrane into highly
ordered macromolecular complexes along with other receptors and signalling proteins …

Quantifying target occupancy of small molecules within living cells

MB Robers, R Friedman-Ohana… - Annual review of …, 2020 - annualreviews.org
The binding affinity and kinetics of target engagement are fundamental to establishing
structure–activity relationships (SARs) for prospective therapeutic agents. Enhancing these …