Results 51 to 60 of about 12,251 (147)

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

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

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

Serotonin 5‐HT7 receptor signaling in neuropsychiatric disorders

Bulletin of the Korean Chemical Society, EarlyView.
5‐HT7R recruits Gs, G12, and β‐arrestin signaling to regulate neuronal plasticity, circuit function, and kinase‐linked intracellular responses. This review summarizes how these pathway‐selective modules contribute to autism spectrum disorder, depression, and schizophrenia, highlighting 5‐HT7R as a pathway‐informed therapeutic target. Abstract Serotonin
Eunseo Park, Hyunah Choo
wiley   +1 more source

Behavioral Characterization of β-Arrestin 1 Knockout Mice in Anxiety-Like and Alcohol Behaviors

Frontiers in Behavioral Neuroscience, 2018
β-Arrestin 1 and 2 are highly expressed proteins involved in the desensitization of G protein-coupled receptor signaling which also regulate a variety of intracellular signaling pathways.
Meridith T. Robins, Terrance Chiang, Jennifer N. Berry, Mee Jung Ko, Jiwon E. Ha, Richard M. van Rijn   +5 more
doaj   +1 more source

Peri-operative opioid analgesia - when is enough too much? A review of opioid-induced tolerance and hyperalgesia [PDF]

, 2019
Opioids are a mainstay of acute pain management but can have many adverse effects, contributing to problematic long-term use. Opioid tolerance (increased dose needed for analgesia) and opioid-induced hyperalgesia (paradoxical increase in pain with opioid
Bull, Fiona, Colvin, Lesley, Hales, Tim
core   +2 more sources

The Serotonin 2B (5‐HT2B) Receptor: A Narrative Review of Preclinical and Clinical Evidence on the Safety Considerations and Therapeutic Potential for the Treatment of Depression

Clinical Pharmacology &Therapeutics, EarlyView.
Major depressive disorder (MDD) and treatment‐resistant depression (TRD) remain leading causes of disability, providing the impetus for receptor‐level treatment strategies beyond monoamine reuptake. The serotonin 5‐HT2B receptor (5‐HT2BR) is uniquely positioned at the interface of central‐antidepressant mechanisms and peripheral cardiac risks.
Gia Han Le, Sabrina Wong, Danica E. Johnson, Diana K. Orsini, Yang Jing Zheng, Kayla M. Teopiz, Christine E. Dri, Joshua D. Rosenblat, Roger S. McIntyre   +8 more
wiley   +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

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