RGD Reference Report - Molecular properties of muscarinic acetylcholine receptors. - Rat Genome Database

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Molecular properties of muscarinic acetylcholine receptors.

Authors: Haga, T 
Citation: Haga T Proc Jpn Acad Ser B Phys Biol Sci. 2013;89(6):226-56.
RGD ID: 8549590
Pubmed: PMID:23759942   (View Abstract at PubMed)
PMCID: PMC3749793   (View Article at PubMed Central)

Muscarinic acetylcholine receptors, which comprise five subtypes (M1-M5 receptors), are expressed in both the CNS and PNS (particularly the target organs of parasympathetic neurons). M1-M5 receptors are integral membrane proteins with seven transmembrane segments, bind with acetylcholine (ACh) in the extracellular phase, and thereafter interact with and activate GTP-binding regulatory proteins (G proteins) in the intracellular phase: M1, M3, and M5 receptors interact with Gq-type G proteins, and M2 and M4 receptors with Gi/Go-type G proteins. Activated G proteins initiate a number of intracellular signal transduction systems. Agonist-bound muscarinic receptors are phosphorylated by G protein-coupled receptor kinases, which initiate their desensitization through uncoupling from G proteins, receptor internalization, and receptor breakdown (down regulation). Recently the crystal structures of M2 and M3 receptors were determined and are expected to contribute to the development of drugs targeted to muscarinic receptors. This paper summarizes the molecular properties of muscarinic receptors with reference to the historical background and bias to studies performed in our laboratories.

Molecular Pathway Annotations    Click to see Annotation Detail View

RGD Manual Annotations

TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
acetylcholine signaling pathway via muscarinic acetylcholine receptor   TAS 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptor   ISOGRK2 (Homo sapiens)8549590; 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptors engaging G alphai protein family  TAS 8549590; 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptors engaging G alphai protein family  ISOGNAI1 (Homo sapiens)8549590; 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptors engaging G alphai protein family  ISOGNAI2 (Homo sapiens)8549590; 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptors engaging G alphaq protein family  TAS 8549590; 8549590; 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptors engaging G alphaq protein family  ISOGNA11 (Homo sapiens)8549590; 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptors engaging G alphaq protein family  ISOGNA14 (Homo sapiens)8549590; 8549590 RGD 
acetylcholine signaling pathway via muscarinic acetylcholine receptors engaging G alphaq protein family  ISOGNAQ (Homo sapiens)8549590; 8549590 RGD 
G protein mediated signaling pathway via Galphai family  TAS 8549590; 8549590 RGD 
G protein mediated signaling pathway via Galphai family  ISOGNAI1 (Homo sapiens)8549590; 8549590 RGD 
G protein mediated signaling pathway via Galphai family  ISOGNAI2 (Homo sapiens)8549590; 8549590 RGD 
G protein mediated signaling pathway via Galphaq family  TAS 8549590; 8549590; 8549590 RGD 
G protein mediated signaling pathway via Galphaq family  ISOGNA11 (Homo sapiens)8549590; 8549590 RGD 
G protein mediated signaling pathway via Galphaq family  ISOGNA14 (Homo sapiens)8549590; 8549590 RGD 
G protein mediated signaling pathway via Galphaq family  ISOGNAQ (Homo sapiens)8549590; 8549590 RGD 
Objects Annotated

Genes (Rattus norvegicus)
Gna11  (G protein subunit alpha 11)
Gna14  (G protein subunit alpha 14)
Gnai1  (G protein subunit alpha i1)
Gnai2  (G protein subunit alpha i2)
Gnaq  (G protein subunit alpha q)
Grk2  (G protein-coupled receptor kinase 2)

Genes (Mus musculus)
Gna11  (guanine nucleotide binding protein, alpha 11)
Gna14  (guanine nucleotide binding protein, alpha 14)
Gnai1  (G protein subunit alpha i1)
Gnai2  (G protein subunit alpha i2)
Gnaq  (guanine nucleotide binding protein, alpha q polypeptide)
Grk2  (G protein-coupled receptor kinase 2)

Genes (Homo sapiens)
GNA11  (G protein subunit alpha 11)
GNA14  (G protein subunit alpha 14)
GNAI1  (G protein subunit alpha i1)
GNAI2  (G protein subunit alpha i2)
GNAQ  (G protein subunit alpha q)
GRK2  (G protein-coupled receptor kinase 2)


Additional Information