Results 51 to 60 of about 29,472 (148)

Functional selectivity of EM-2 analogs at the mu-opioid receptor

Frontiers in Pharmacology, 2023
The mu opioid receptor agonists are the most efficacious pain controlling agents but their use is accompanied by severe side effects. More recent developments indicate that some ligands can differentially activate receptor downstream pathways, possibly ...
Justyna Piekielna-Ciesielska, Davide Malfacini, Francine Medjiofack Djeujo, Chantal Marconato, Karol Wtorek, Girolamo Calo’, Anna Janecka   +6 more
doaj   +1 more source

Quinolones modulate ghrelin receptor signaling: potential for a novel small molecule scaffold in the treatment of cachexia [PDF]

, 2018
Cachexia is a metabolic wasting disorder characterized by progressive weight loss, muscle atrophy, fatigue, weakness, and appetite loss. Cachexia is associated with almost all major chronic illnesses including cancer, heart failure, obstructive ...
Cano, Rafael, Juan Rodríguez, Rocío, Kandil, Dalia, McGlacken, Gerard P., Pastor Cavada, Elena, Schellekens, Harriët, Shaban, Hamdy, Shanahan, Rachel, Torres-Fuentes, Cristina   +8 more
core   +3 more sources

Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities

Molecules, 2021
The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed.
Yazan J. Meqbil, Hongyu Su, Robert J. Cassell, Kendall L. Mores, Anna M. Gutridge, Benjamin R. Cummins, Lan Chen, Richard M. van Rijn   +7 more
doaj   +1 more source

Editorial [PDF]

, 2016
No abstract ...
Baillie, George S.
core   +1 more source

Signaling bias of the protease-activated receptor-1 is dictated by distinct GRK5 and β-arrestin-2 determinants

Cell Reports
Summary: G protein-coupled receptors (GPCRs) exhibit signaling bias or preferential activation of heterotrimeric G proteins versus GPCR kinase (GRK)-mediated β-arrestin signaling.
Monica L. Gonzalez Ramirez, Lennis B. Orduña-Castillo, Carolyne Bardeleben, Huaping Qin, Ying Lin, Cierra A. Birch, Irina Kufareva, JoAnn Trejo   +7 more
doaj   +1 more source

Biased signaling of the angiotensin II type 1 receptor can be mediated through distinct mechanisms. [PDF]

PLoS ONE, 2010
Seven transmembrane receptors (7TMRs) can adopt different active conformations facilitating a selective activation of either G protein or β-arrestin-dependent signaling pathways.
Marie Mi Bonde, Jonas Tind Hansen, Samra Joke Sanni, Stig Haunsø, Steen Gammeltoft, Christina Lyngsø, Jakob Lerche Hansen   +6 more
doaj   +1 more source

The α-arrestin ARRDC3 mediates ALIX ubiquitination and G protein-coupled receptor lysosomal sorting. [PDF]

, 2015
The sorting of G protein-coupled receptors (GPCRs) to lysosomes is critical for proper signaling and cellular responses. We previously showed that the adaptor protein ALIX regulates lysosomal degradation of protease-activated receptor-1 (PAR1), a GPCR ...
Dores, Michael R, J Grimsey, Neil, Lin, Huilan, Mendez, Francisco, Trejo, JoAnn   +4 more
core   +1 more source

Effect of penehyclidine hydrochloride on -arrestin-1 expression in lipopolysaccharide-induced human pulmonary microvascular endothelial cells

Brazilian Journal of Medical and Biological Research, 2013
β-arrestins are expressed proteins that were first described, and are well-known, as negative regulators of G protein-coupled receptor signaling.
J. Zhan, F. Xiao, Z.Z. Zhang, Y.P. Wang, K. Chen, Y.L. Wang   +5 more
doaj   +1 more source

Inhibitory Effect of CCK-8 on Methamphetamine-Induced Apoptosis

Fayixue Zazhi, 2021
ObjectiveTo investigate the inhibitory effect of cholecystokinin octapeptide （CCK-8） binding to cholecystokinin 2 receptor （CCK2R） on methamphetamine （METH）-induced neuronal apoptosis, and to explore the signal transduction mechanism of β-arrestin 2 in ...
ZHANG Wu-hua, ZHANG Ming-long, JING Wei-wei, XIE Bing, BI Hai-tao, YU Feng, CONG Bin, MA Chun-ling, WEN Di   +8 more
doaj   +1 more source

Pepducin-mediated cardioprotection via β-arrestin-biased β2-adrenergic receptor-specific signaling [PDF]

, 2018
Reperfusion as a therapeutic intervention for acute myocardial infarction-induced cardiac injury itself induces further cardiomyocyte death. β-arrestin (βarr)-biased β-adrenergic receptor (βAR) activation promotes survival signaling responses in vitro ...
Benovic, Jeffrey L., Carter, Rhonda L., de Lucia, Claudio, Gao, Erhe, Grisanti, Laurel A., Koch, Walter J., Thomas, Toby P., Tilley, Douglas G.   +7 more
core   +1 more source