Inhibition of the Proliferation of Human Lung Fibroblasts by Prostacyclin Receptor Agonists is Linked to a Sustained cAMP Signal in the Nucleus

Autor: Maxine J. Roberts, Lauren T. May, Alastair C. Keen, Bonan Liu, Terrance Lam, Steven J. Charlton, Elizabeth M. Rosethorne, Michelle L. Halls

Publikováno v: Frontiers in Pharmacology, Vol 12 (2021)

Idiopathic pulmonary fibrosis is a chronic and progressive fibrotic lung disease, and current treatments are limited by their side effects. Proliferation of human lung fibroblasts in the pulmonary interstitial tissue is a hallmark of this disease and

Externí odkaz: https://doaj.org/article/5c85396c76d64dc79fc084910f1ff65a

The inhibition of human lung fibroblast proliferation and differentiation by Gs-coupled receptors is not predicted by the magnitude of cAMP response

Autor: Maxine J. Roberts, Rebecca E. Broome, Toby C. Kent, Steven J. Charlton, Elizabeth M. Rosethorne

Publikováno v: Respiratory Research, Vol 19, Iss 1, Pp 1-13 (2018)

Abstract Background Idiopathic pulmonary fibrosis (IPF) is 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, n

Externí odkaz: https://doaj.org/article/06e8bdf96a7a40f48b463226c6ba76c7

Mass spectrometry captures biased signalling and allosteric modulation of a G-protein-coupled receptor

Autor: Hsin-Yung Yen, Idlir Liko, Wanling Song, Parth Kapoor, Fernando Almeida, Joanna Toporowska, Karolina Gherbi, Jonathan T. S. Hopper, Steven J. Charlton, Argyris Politis, Mark S. P. Sansom, Ali Jazayeri, Carol V. Robinson

Publikováno v: Nature Chemistry. 14:1375-1382

G-protein-coupled receptors signal through cognate G proteins. Despite the widespread importance of these receptors, their regulatory mechanisms for G-protein selectivity are not fully understood. Here we present a native mass spectrometry-based appr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ffd0d1680a992e84a4470b8de796b752
https://doi.org/10.1038/s41557-022-01041-9

The role of kinetic context in apparent biased agonism at GPCRs

Autor: Carmen Klein Herenbrink, David A. Sykes, Prashant Donthamsetti, Meritxell Canals, Thomas Coudrat, Jeremy Shonberg, Peter J. Scammells, Ben Capuano, Patrick M. Sexton, Steven J. Charlton, Jonathan A. Javitch, Arthur Christopoulos, J. Robert Lane

Publikováno v: Nature Communications, Vol 7, Iss 1, Pp 1-14 (2016)

Biased agonists act at a receptor to preferentially induce distinct intracellular signalling responses over others. Here the authors show how kinetics of ligand binding and signaling responses greatly influence observed bias profiles, and hence must

Externí odkaz: https://doaj.org/article/0783ff6940594b04b8cd38d7c0762fb1

Interaction With the Lipid Membrane Influences Fentanyl Pharmacology

Autor: Katy J. Sutcliffe, Robin A Corey, Norah Alhosan, Damiana Cavallo, Sam Groom, Marina Santiago, Chris Bailey, Steven J. Charlton, Richard B. Sessions, Graeme Henderson, Eamonn Kelly

Publikováno v: Sutcliffe, K J, Corey, R A, Alhosan, N, Cavallo, D, Groom, S, Santiago, M, Bailey, C, Charlton, S J, Sessions, R B, Henderson, G & Kelly, E 2022, ' Interaction With the Lipid Membrane Influences Fentanyl Pharmacology ', Advances in drug and alcohol research, vol. 2, 10280 . https://doi.org/10.3389/adar.2022.10280

Overdose deaths from fentanyl have reached epidemic proportions in the USA and are increasing worldwide. Fentanyl is a potent opioid agonist that is less well reversed by naloxone than morphine. Due to fentanyl’s high lipophilicity and elongated st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::333656ded7415d571fa1ae68f2a11c89
https://doi.org/10.3389/adar.2022.10280