Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes [PDF]
Science, 2019 Choosing a partner G protein–coupled receptors (GPCRs) bind ligands outside the cell and trigger events inside the cell by selectively binding and activating specific G proteins. The selectivity occurs even among highly related GPCRs.
Shoji Maeda +4 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 ...
Haga, Kazuko +10 more
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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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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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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.
R, Pals-Rylaarsdam +4 more
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Unraveling a molecular determinant for clathrin-independent internalization of the M2 muscarinic acetylcholine receptor [PDF]
Scientific Reports, 2015 AbstractEndocytosis and postendocytic sorting of G-protein-coupled receptors (GPCRs) is important for the regulation of both their cell surface density and signaling profile. Unlike the mechanisms of clathrin-dependent endocytosis (CDE), the mechanisms underlying the control of GPCR signaling by clathrin-independent endocytosis (CIE) remain largely ...
Wan, Min +6 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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The structure of the third intracellular loop of the muscarinic acetylcholine receptor M2 subtype [PDF]
FEBS Letters, 2005 We have examined whether the long third intracellular loop (i3) of the muscarinic acetylcholine receptor M2 subtype has a rigid structure. Circular dichroism (CD) and nuclear magnetic resonance spectra of M2i3 expressed in and purified from Escherichia coli indicated that M2i3 consists mostly of random coil.
Ichlyama, S +6 more
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Internalization and Down-regulation of Human Muscarinic Acetylcholine Receptor m2 Subtypes [PDF]
Journal of Biological Chemistry, 1998 Internalization and down-regulation of human muscarinic acetylcholine m2 receptors (hm2 receptors) and a hm2 receptor mutant lacking a central part of the third intracellular loop (I3-del m2 receptor) were examined in Chinese hamster ovary (CHO-K1) cells
Hirofumi Tsuga +5 more
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