M2 Muscarinic acetylcholine receptor modulates rat airway smooth muscle cell proliferation [PDF]
World Allergy Organization Journal, 2013 Airways chronic inflammatory conditions in asthma and COPD are characterized by tissue remodeling, being smooth muscle hyperplasia, the most important feature.
Fabiola A. Placeres-Uray +5 more
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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.
Aaron G. Roseberry +1 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
Hiroyasu Furukawa, Tatsuya 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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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 ...
Kazuko Haga +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 ...
Jesús Gomeza +8 more
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Desensitization and Internalization of the m2 Muscarinic Acetylcholine Receptor Are Directed by Independent Mechanisms [PDF]
Journal of Biological Chemistry, 1995 The phenomenon of acute desensitization of G-protein-coupled receptors has been associated with several events, including receptor phosphorylation, loss of high affinity agonist binding, receptor:G-protein uncoupling, and receptor internalization.
Robin Pals‐Rylaarsdam +4 more
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An allosteric ligand stabilizes distinct conformations in the M2 muscarinic acetylcholine receptor [PDF]
, 2021 AbstractAllosteric modulators provide therapeutic advantages over orthosteric drugs. A plethora of allosteric modulators have been identified for several GPCRs, particularly for muscarinic receptors (mAChRs)1,2. To study the molecular mechanisms governing allosteric modulation, we utilized a recently developed NMR system to investigate the ...
Jun Xu +6 more
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Synergistic regulation mechanism of iperoxo and LY2119620 for muscarinic acetylcholine M2 receptor
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, Haifeng Chen
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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.
Gerhard Wolber, Marcel Bermudez
openaire +2 more sources