Results 51 to 60 of about 29,885 (192)

Cannabinoid CB1 and CB2 Receptor-Mediated Arrestin Translocation: Species, Subtype, and Agonist-Dependence

Frontiers in Pharmacology, 2019
Arrestin translocation and signaling have come to the fore of the G protein-coupled receptor molecular pharmacology field. Some receptor–arrestin interactions are relatively well understood and considered responsible for specific therapeutic or adverse ...
Mikkel Søes Ibsen, Mikkel Søes Ibsen, David B. Finlay, Monica Patel, Monica Patel, Jonathan A. Javitch, Jonathan A. Javitch, Michelle Glass, Natasha Lillia Grimsey, Natasha Lillia Grimsey   +9 more
doaj   +1 more source

Loss of biased signaling at a G protein-coupled receptor in overexpressed systems.

PLoS ONE, 2023
G protein-coupled receptors (GPCRs) regulate cellular signaling pathways by coupling to two classes of transducers: heterotrimeric G proteins and β-arrestins.
Angus Li, Samuel Liu, Rennica Huang, Seungkirl Ahn, Robert J Lefkowitz   +4 more
doaj   +1 more source

T Cell Exhaustion in Cancer Immunotherapy: Heterogeneity, Mechanisms, and Therapeutic Opportunities

Advanced Science, EarlyView.
T cell exhaustion limits immunotherapy efficacy. This article delineates its progression from stem‐like to terminally exhausted states, governed by persistent antigen, transcription factors, epigenetics, and metabolism. It maps the exhaustion landscape in the TME and proposes integrated reversal strategies, providing a translational roadmap to overcome
Yang Yu, Xiaoyu Yao, Qingyang Wang, Mengrui Yang, Runze Li, Jiangjiang Qin, Jing Zhuang, Changgang Sun   +7 more
wiley   +1 more source

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

Divergent Roles of mGlu2 and mGlu3 Receptors in Amyloid‐β Production and Cognitive Dysfunctions in Alzheimer's Disease

Advanced Science, EarlyView.
This study explores the opposing effects of the mGluR2 and mGluR3 receptors on amyloid precursor protein processing. mGluR2 promotes amyloidogenic cleavage, while mGluR3 favors non‐amyloidogenic pathways. Using a brain‐penetrant nanobody as a mGluR2 positive allosteric modulator, the study uncovers how its chronic activation aggravates amyloid‐β burden
Pierre‐André Lafon, Mireille Elodie Tsitokana, Ugo Guy Alenda, Yen‐Ling Lian, Clémentine Eva Philibert, Mathieu Oosterlaken, Marta Cimadevila, Gaëlle Dudon, Jessica Monnic, Salomé Roux, Julie Bessié, Séverine Diem, Franck Vandermoere, Laurent Prézeau, Patrick Chames, Julie Kniazeff, Sylvie Claeysen, Anaïs Menny, Jean‐Philippe Pin, Véronique Perrier, Jianfeng Liu, Philippe Rondard   +21 more
wiley   +1 more source

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

Tailoring therapy for heart failure: the pharmacogenomics of adrenergic receptor signaling. [PDF]

, 2014
Heart failure is one of the leading causes of mortality in Western countries, and β-blockers are a cornerstone of its treatment. However, the response to these drugs is variable among individuals, which might be explained, at least in part, by genetic ...
Barrese, V, Femminella, GD, Ferrara, N, Rengo, G   +3 more
core   +2 more sources

Nano‐Gs‐Protein Peptidomimetika: Rationales Design von Peptiden, die vom C‐Terminus von Gα abgeleitet sind und Schlüsselkomponenten der Gs‐β2AR‐Wechselwirkungen nachahmen

Angewandte Chemie, EarlyView.
G Protein‐gekoppelte Rezeptoren (GPCRs) sind wichtige therapeutische Zielstrukturen. Die Modulation der GPCR‐Aktivität über intrazelluläre Bindungsstellen gewinnt zunehmend an Bedeutung. Ein strukturell und computergestützter Ansatz ermöglichte die Entwicklung kleiner, vom G Protein abgeleiteter Peptidomimetika, die gezielt an die intrazelluläre ...
Phuong Thu Tran, Mia Danielsen, Johanna K. S. Tiemann, Passainte Ibrahim, Søren G. F. Rasmussen, Xavier Kubiak, Hossein Batebi, Charlène Gadais, Steven Ballet, Peter W. Hildebrand, Daniel Sejer Pedersen, Jesper Mosolff Mathiesen   +11 more
wiley   +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

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