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All Outputs (5)

Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations (2018)
Journal Article
Civciristov, S., Ellisdon, A. M., Suderman, R., Pon, C. K., Evans, B. A., Kleifeld, O., …Halls, M. L. (2018). Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations. Science Signaling, 11(551), Article eaan1188. https://doi.org/10.1126/scisignal.aan1188

G protein–coupled receptors (GPCRs) are the largest class of cell surface signaling proteins, participate in nearly all physiological processes, and are the targets of 30% of marketed drugs. Typically, nanomolar to micromolar concentrations of ligand... Read More about Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations.

The inhibition of human lung fibroblast proliferation and differentiation by Gs-coupled receptors is not predicted by the magnitude of cAMP response (2018)
Journal Article
Roberts, M. J., Broome, R. E., Kent, T. C., Charlton, S. J., & Rosethorne, E. M. (2018). The inhibition of human lung fibroblast proliferation and differentiation by Gs-coupled receptors is not predicted by the magnitude of cAMP response. Respiratory Research, 19, Article 56. https://doi.org/10.1186/s12931-018-0759-2

Background Idiopathic pulmonary fibrosis (IPF) is 22 a chronic and progressive fibrotic lung disease for which there is no cure. Current therapeutics are only able to slow disease progression, therefore there is a need to explore alternative, novel t... Read More about The inhibition of human lung fibroblast proliferation and differentiation by Gs-coupled receptors is not predicted by the magnitude of cAMP response.

Biased agonism in drug discovery: is it too soon to choose a path? (2018)
Journal Article
Michel, M. C., & Charlton, S. J. (2018). Biased agonism in drug discovery: is it too soon to choose a path?. Molecular Pharmacology, 93(4), https://doi.org/10.1124/mol.117.110890

A single receptor can activate multiple signaling pathways that have distinct or even opposite effects on cell function. Biased agonists stabilize receptor conformations preferentially stimulating one of these pathways, and therefore allow a more tar... Read More about Biased agonism in drug discovery: is it too soon to choose a path?.

Micro-pharmacokinetics: quantifying local drug concentration at live cell membranes (2018)
Journal Article
Gherbi, K., Briddon, S. J., & Charlton, S. J. (in press). Micro-pharmacokinetics: quantifying local drug concentration at live cell membranes. Scientific Reports, 8, Article 3479. https://doi.org/10.1038/s41598-018-21100-x

Fundamental equations for determining pharmacological parameters, such as the binding afnity of a ligand for its target receptor, assume a homogeneous distribution of ligand, with concentrations in the immediate vicinity of the receptor being the sam... Read More about Micro-pharmacokinetics: quantifying local drug concentration at live cell membranes.