Results 81 to 90 of about 58,465 (248)

Engineering of three-finger fold toxins creates ligands with original pharmacological profiles for muscarinic and adrenergic receptors. [PDF]

PLoS ONE, 2012
Protein engineering approaches are often a combination of rational design and directed evolution using display technologies. Here, we test "loop grafting," a rational design method, on three-finger fold proteins.
Carole Fruchart-Gaillard, Gilles Mourier, Guillaume Blanchet, Laura Vera, Nicolas Gilles, Renée Ménez, Elodie Marcon, Enrico A Stura, Denis Servent   +8 more
doaj   +1 more source

Pharmacological and Mechanistic Interventions for Cognitive Impairment Associated With Schizophrenia: A Review of Registered Clinical Trials

Acta Psychiatrica Scandinavica, EarlyView.
ABSTRACT Background Schizophrenia is characterized by positive, negative, and cognitive symptoms. Current pharmacological treatments often fail to address cognitive deficits. In this review of clinical trials, we aim to identify studies that explore neurobiological (non‐psychological) strategies to address Cognitive Impairment Associated with ...
Bahareh Peyrovian, Lena Palaniyappan, Theodore T. Kolivakis, Howard C. Margolese   +3 more
wiley   +1 more source

Molecular Mechanisms of Bitopic Ligand Engagement with the M1 Muscarinic Acetylcholine Receptor*

Journal of Biological Chemistry, 2014
Background: Bitopic ligands bind concomitantly to orthosteric and allosteric receptor sites. Results: Residues affecting binding and biased signaling of the selective agonists TBPB and 77-LH-28-1 were identified at the M1 muscarinic receptor. Conclusion:
Peter Keov, Laura Lopez, Shane M. Devine, C. Valant, J. R. Lane, P. Scammells, P. Sexton, A. Christopoulos   +7 more
semanticscholar   +1 more source

Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]

, 2007
Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung, Li, Bo, Scarselli, Marco, Wess, Jürgen   +3 more
core   +1 more source

Acetylcholine From Solitary Chemosensory Cell, Not Neuron, Regulates Basal Cell Fate Driving Eosinophilic Chronic Rhinosinusitis With Nasal Polyps

Allergy, EarlyView.
This study identifies that Ach levels are elevated in eCRSwNP and primarily released from SCCs rather than neurons. Ach induces epithelial remodeling in eCRSwNP by binding to M1R/M3R and activating YAP signaling in basal cells, driving basal cell hyperplasia and abnormal differentiation. Blocking M1R/M3R with TB inhibits eCRSwNP progression.
Bowen Zheng, Tao Lu, Ji Wang, Yalan Zhang, Panhui Xiong, Jieyu Zeng, Shuman Li, Yu Jiang, Yijun Liu, Longlan Shu, Yuan Chen, Yin Zhou, Yue Gu, Dayu Guan, Chenxi Li, Lei Zhao, Shujin Wang, Jie Liu, Xia Ke, Yang Shen, Yucheng Yang   +20 more
wiley   +1 more source

Cholinergic regulation of mood: from basic and clinical studies to emerging therapeutics. [PDF]

, 2019
Mood disorders are highly prevalent and are the leading cause of disability worldwide. The neurobiological mechanisms underlying depression remain poorly understood, although theories regarding dysfunction within various neurotransmitter systems have ...
Dulawa, Stephanie C, Janowsky, David S
core  

Inhibition of Connexin43 hemichannels impairs spatial short-term memory without affecting spatial working memory [PDF]

, 2016
Astrocytes are active players in higher brain function as they can release gliotransmitters, which are essential for synaptic plasticity. Various mechanisms have been proposed for gliotransmission, including vesicular mechanisms as well as non-vesicular ...
Albertini, Giulia, De Bundel, Dimitri, Leybaert, Luc, Smolders, Ilse J., Vinken, Mathieu, Walrave, Laura   +5 more
core   +2 more sources

State‐dependent regulation of the Kv7.2 channel voltage sensor by QO‐58

British Journal of Pharmacology, EarlyView.
Background and Purpose KV7(KCNQ) potassium channels are key modulators of neuronal excitability, and promising targets for development of drugs for epilepsy and pain. We investigated a candidate KV7 drug, QO‐58, which has been previously described but has an unclear mechanism of action.
Richard Kanyo, Shawn M. Lamothe, Thomas M. Hammond, Harley T. Kurata   +3 more
wiley   +1 more source

Allosteric Modulation of M1 Muscarinic Acetylcholine Receptor Internalization and Subcellular Trafficking*

Journal of Biological Chemistry, 2014
Background: The effects of allosteric modulators on G protein-coupled receptor trafficking are largely unknown. Results: The allosteric ligand BQCA modulates M1 mAChR arrestin recruitment and receptor trafficking.
Holly R. Yeatman, J. R. Lane, K. H. C. Choy, N. Lambert, P. Sexton, A. Christopoulos, Meritxell Canals   +6 more
semanticscholar   +1 more source

The varieties of the psychedelic experience: A preliminary study of the association between the reported subjective effects and the binding affinity profiles of substituted phenethylamines and tryptamines [PDF]

, 2018
Classic psychedelics are substances of paramount cultural and neuroscientific importance. A distinctive feature of psychedelic drugs is the wide range of potential subjective effects they can elicit, known to be deeply influenced by the internal state of
Erowid, Earth, Erowid, Fire, Martínez Vivot, Rocío, Pallavicini, Carla, Sanz, Camila, Tagliazucchi, Enzo Rodolfo, Zamberlan, Federico   +6 more
core   +2 more sources