Results 1 to 10 of about 8,008 (118)
Non-Neuronal Functions of the M2 Muscarinic Acetylcholine Receptor [PDF]
Genes, 2013 Acetylcholine is an important neurotransmitter whose effects are mediated by two classes of receptors. The nicotinic acetylcholine receptors are ion channels, whereas the muscarinic receptors belong to the large family of G protein coupled seven transmembrane helix receptors.
Ritva Tikkanen +2 more
exaly +5 more sources
Dualsteric modulators of the M2 muscarinic acetylcholine receptor [PDF]
Journal of Cheminformatics, 2014 G-protein coupled receptors (GPCRs) trigger multiple signal-switching mechanisms like binding of s-arrestin proteins, activation of kinases and G-protein activation [1]. The poor understanding of the conformational changes resulting in these activations is a major challenge for the design of specific GPCR modulating drugs.
Marcel Bermudez, Gerhard Wolber
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Revisiting the Endocytosis of the M2 Muscarinic Acetylcholine Receptor [PDF]
Membranes, 2015 The agonist-induced endocytosis of the muscarinic acetylcholine receptor M2 is different from that of the other members of the muscarinic receptor family. The uptake of the M2 receptor involves the adapter proteins of the β-arrestin family and the small GTPase ADP-ribosylation factor 6.
Wymke Ockenga, Ritva Tikkanen
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Trafficking of M2 Muscarinic Acetylcholine Receptors [PDF]
Journal of Biological Chemistry, 1999 Internalization is an important mechanism regulating the agonist-dependent responses of G-protein-coupled receptors. The internalization of the M(2) muscarinic cholinergic receptors (mAChR) in HEK293 cells has been demonstrated to occur by an unknown mechanism that is independent of arrestins and dynamin.
A G, Roseberry, M M, Hosey
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On homology modeling of the M2 muscarinic acetylcholine receptor subtype [PDF]
Journal of Computer-Aided Molecular Design, 2013 Twelve homology models of the human M(2) muscarinic receptor using different sets of templates have been designed using the Prime program or the modeller program and compared to crystallographic structure (PDB:3UON). The best models were obtained using single template of the closest published structure, the M(3) muscarinic receptor (PDB:4DAJ).
Jan Jakubik +2 more
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Expression of Functional M2 Muscarinic Acetylcholine Receptor in Escherichia coli [PDF]
Journal of Biochemistry, 2000 The M2 muscarinic acetylcholine receptor mutant (M2 mutant), with a lack of glycosylation sites, a deletion in the central part of the third inner loop, and the addition of a six histidine tag at the C-terminus, was fused to maltose binding protein (MBP) at its N-terminus and expressed in Escherichia coli. The expression level was 0.2 nmol receptor per
H, Furukawa, T, Haga
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Modulation of the M2 Muscarinic Acetylcholine Receptor Activity with Monoclonal Anti-M2 Receptor Antibody Fragments [PDF]
Journal of Biological Chemistry, 2004 Antibodies directed against the second extracellular loop of G protein-coupled receptors are known to have functional activities. From a partial agonist monoclonal antibody directed against the M2 muscarinic receptor, we constructed and produced a single chain variable fragment with high affinity for its target epitope.
Jean-Christophe, Peter +6 more
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Synergistic regulation mechanism of iperoxo and LY2119620 for muscarinic acetylcholine M2 receptor [PDF]
RSC Advances, 2018 Dynamics correlation network was used to reveal the synergistic regulation mechanism of iperoxo and LY2119620 for muscarinic acetylcholine M2 receptor.
Quan Li, Hai-Feng Chen
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Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist [PDF]
Nature, 2012 The parasympathetic branch of the autonomic nervous system regulates the activity of multiple organ systems. Muscarinic receptors are G-protein-coupled receptors that mediate the response to acetylcholine released from parasympathetic nerves. Their role in the unconscious regulation of organ and central nervous system function makes them potential ...
Haga, Kazuko +10 more
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Pronounced pharmacologic deficits in M2 muscarinic acetylcholine receptor knockout mice [PDF]
Proceedings of the National Academy of Sciences, 1999 Members of the muscarinic acetylcholine receptor family (M1–M5) are known to be involved in a great number of important central and peripheral physiological and pathophysiological processes. Because of the overlapping expression patterns of the M1–M5 muscarinic receptor subtypes and the lack of ligands endowed with sufficient subtype selectivity ...
J, Gomeza +8 more
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