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, Hai-Feng Chen
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Cardiology Research and Practice, 2019 Objectives. To investigate the association of serum autoantibodies against M2-muscarinic acetylcholine receptor (anti-M2-R) with atrial fibrosis in long-standing persistent atrial fibrillation (AF) patients. Methods.
Guiling Ma +6 more
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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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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 ...
Changwen Jin +8 more
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Safety and tolerability of the M2 muscarinic acetylcholine receptor modulator BAY 2413555 in heart failure with reduced ejection fraction in the REMOTE-HF study. [PDF]
Sci RepBAY 2413555 is a novel selective and reversible positive allosteric modulator of the type 2 muscarinic acetylcholine (M2) receptor, aimed at enhancing parasympathetic signaling and restoring cardiac autonomic balance for the treatment of heart failure ...
Fudim M +10 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 ...
Tao Xu +6 more
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Porcine m2 Muscarinic Acetylcholine Receptor-Effector Coupling in Chinese Hamster Ovary Cells [PDF]
Journal of Biological Chemistry, 1995 The relationship between porcine m2 muscarinic receptor coupling to inhibition of cAMP formation and stimulation of phosphatidylinositol metabolism in Chinese hamster ovary cells was examined. Reduction of the number of receptors per cell with the slowly dissociating antagonist (-)-quinuclidinyl benzilate caused a decrease in maximal response with no ...
Dylan A. Bulseco +3 more
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BK Channels Regulate Contraction Secondary to M2 Muscarinic Acetylcholine Receptor Mediated Depolarization [PDF]
Biophysical Journal, 2011 Airway smooth muscles (ASM) contraction is primarily mediated by M2 and M3 muscarinic acetylcholine receptors. We and others have shown that one of the functions of large conductance Ca2+- and voltage-activated (BK) potassium channel and the accessory β1 subunit is to moderate ASM excitation-contraction coupling by opposing cholinergic evoked ...
Bin Wang +3 more
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Muscarinic receptor regulation of chronic pain-induced atrial fibrillation
Frontiers in Cardiovascular Medicine, 2022 Atrial fibrillation (AF), one of the most common arrhythmias, is associated with chronic emotional disorder. Chronic pain represents a psychological instability condition related to cardiovascular diseases, but the mechanistic linkage connecting chronic ...
Chao Gong +10 more
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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
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