Results 21 to 30 of about 18,227 (256)

Novel Interaction between the M4 Muscarinic Acetylcholine Receptor and Elongation Factor 1A2 [PDF]

open access: hybridJournal of Biological Chemistry, 2002
The activation of the muscarinic acetylcholine receptor (mAChR) family, consisting of five subtypes (M1-M5), produces a variety of physiological effects throughout the central nervous system. However, the role of each individual subtype remains poorly understood.
Daniel B. McClatchy   +5 more
openalex   +6 more sources

Allosteric Modulators of the M4 Muscarinic Acetylcholine Receptor

open access: greenACS Medicinal Chemistry Letters, 2017
Summary: Acetylcholine (ACh) is a neurotransmitter that is hydrolyzed by the enzyme cholinesterase into chlorine and acetic acid. ACh is expressed at all autonomic ganglia, automomic nervous system, sweat glands, sympathetic automomic nervous system ...
Robert B. Kargbo
openalex   +2 more sources

In vitro evaluation of PET radiotracers for imaging synaptic density, the acetylcholine transporter, AMPA-tarp-γ8 and muscarinic M4 receptors in Alzheimer’s disease

open access: bronzeAmerican Journal of Nuclear Medicine and Molecular Imaging
Several therapeutics and biomarkers that target Alzheimer's disease (AD) are under development. Our clinical positron emission tomography (PET) research programs are interested in six radiopharmaceuticals to image patients with AD and related dementias ...
Faustine d’Orchymont
openalex   +2 more sources

Coincidence detection at the level of phospholipase C activation mediated by the m4 muscarinic acetylcholine receptor [PDF]

open access: bronzeCurrent Biology, 1995
One of the principal mechanisms by which G-protein-coupled receptors evoke cellular responses is through the activation of phospholipase C (PLC) and the subsequent release of Ca2+ from intracellular stores. Receptors that couple to pertussis toxin (PTX)-insensitive G proteins typically evoke large increases in PLC activity and intracellular Ca2 ...
Reed C. Carroll   +2 more
openalex   +4 more sources

Downstream Signaling of Muscarinic M<sub>4</sub> Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]

open access: yesPharmacol Res Perspect
ABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M   +5 more
europepmc   +2 more sources

CaMKIIα, a modulator of M4 muscarinic acetylcholine receptors

open access: goldCommunicative & Integrative Biology, 2010
G protein-coupled receptors (GPCRs) are subject to the regulation by protein kinases. By controlling the phosphorylation-dephosphorylation balance, protein kinases actively modify GPCR expression and function. In a recent study, we have identified a novel phosphorylation-dependent regulation of Gαi/o-coupled muscarinic acetylcholine receptors.
Ming‐Lei Guo   +4 more
openalex   +4 more sources

Modulation of M4 muscarinic acetylcholine receptors by interacting proteins

open access: greenNeuroscience Bulletin, 2010
Protein-protein interactions represent an important mechanism for posttranslational modifications of protein expression and function. In brain cells, surface-expressed and membrane-bound neurotransmitter receptors are common proteins that undergo dynamic protein-protein interactions between their intracellular domains and submembranous regulatory ...
Ming‐Lei Guo, Li-Min Mao, John Q. Wang
openalex   +5 more sources

Structural Determinants of Allosteric Agonism and Modulation at the M4 Muscarinic Acetylcholine Receptor [PDF]

open access: hybridJournal of Biological Chemistry, 2010
The recently identified small molecule, 3-amino-5-chloro-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxylic acid cyclopropylamide (LY2033298), is the first selective allosteric modulator of the muscarinic acetylcholine receptors (mAChRs) that mediates both receptor activation and positive modulation of the endogenous agonist, acetylcholine (ACh), via
Vindhya Nawaratne   +4 more
openalex   +5 more sources

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