Vibrational analysis of acetylcholine binding to the M2 receptor
نویسندگان
چکیده
منابع مشابه
A fluorophore attached to nicotinic acetylcholine receptor M2 detects productive binding of agonist to the site
To study conformational transitions at the muscle nicotinic acetylcholine (ACh) receptor (nAChR), a rhodamine fluorophore was tethered to a Cys side chain introduced at the 19 position in the M2 region of the nAChR expressed in Xenopus oocytes. This procedure led to only minor changes in receptor function. During agonist application, fluorescence increased by ( F F) 10%, and the emission peak s...
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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. However, it has remained inconclusive if M2 endocytosis is dependent on clathrin or the large GTPase dynamin....
متن کاملDualsteric modulators of the M2 muscarinic acetylcholine receptor
G-protein coupled receptors (GPCRs) trigger multiple signal-switching mechanisms like binding of ß-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. For the muscarinic M2 receptor, allosteric, orthosteric and dualsteric b...
متن کاملOn homology modeling of the M2 muscarinic acetylcholine receptor subtype
Twelve homology models of the human M2 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 M3 muscarinic receptor (PDB:4DAJ). Adding more (structurally distant) templates led to wor...
متن کاملNon-Neuronal Functions of the M2 Muscarinic Acetylcholine Receptor
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. Beyond its function in neuronal systems, it has become evident that acetylcholine also plays an important role in non-ne...
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ژورنال
عنوان ژورنال: RSC Advances
سال: 2021
ISSN: 2046-2069
DOI: 10.1039/d1ra01030a