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

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors

Autor: David A. Sykes, Holly Moore, Lisa Stott, Nicholas Holliday, Jonathan A. Javitch, J. Robert Lane, Steven J. Charlton

Publikováno v: Nature Communications, Vol 8, Iss 1, Pp 1-11 (2017)

Atypical antipsychotics show reduced extrapyramidal side effects compared to first generation drugs. Here the authors use time-resolved FRET to measure binding kinetics, and show that side effects correlate with drug association rates to the D2 recep

Externí odkaz: https://doaj.org/article/92ce2e6b0c464f92849b40c8f8648e24

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

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