Muscarinic acetylcholine receptor

Function Muscarinic acetylcholine receptors (mAChR) contain 5 subtypes M1-M5. Subtypes M1, M3, M5 activate phospholipase C which leads to activation of protein kinase C. M2 and M4 inhibit adenylyl cyclase activity and activate G protein-gated potassium channels. mAChRs belong to the family of rhodopsin-like G protein coupled seven transmembrane helix receptors and perform various non-neuronal functions. Disease mAChR M1 agonists are developed for treatment of Alzheimer disease. M2 antagonists are developed for treatment of Alzheimer disease and M3 antagonists for treatment of overactive bladder and chronic obstructive pulmonary disease Structural highlights Antagonists bind to mAChR M2 at the . The antagonist interacts with protein residues . See also: G protein-coupled receptor Receptor Transmembrane (cell surface) receptors Tiotropium bromide

spinqualitylabelsall models Human muscarinic acetylcholine receptor M2 complex with antagonist (PDB code 5zkb) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

3D Structures of muscarinic acetylcholine receptors3D Structures of muscarinic acetylcholine receptors

Updated on 15-July-2024

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• Muscarinic acetylcholine receptor M1
  • 6oij – hAChR M1 (mutant) + guanine nucleotide-binding protein + antibody fragment + transducing b chain 1 – human – Cryo EM
    
  • 5cxv – hAChR M1 (mutant) + flag peptide + tiotropium
    
  • 6wjc – hAChR M1/endolysin + muscarinic toxin 7
    
  • 6zfz, 6zg4, 6zg9 – hAChR M1 (mutant)/endolysin + agonist
    
• Muscarinic acetylcholine receptor M2
  • 3uon, 5zk3, 5zk8, 5zkb, 5zkc, 5yc8 – hAChR M2 (mutant) + antagonist
    
  • 4mqs – hAChR M2 (mutant) + nanobody + iperoxo
    
  • 4mqt – hAChR M2 (mutant) + nanobody + iperoxo + modulator
    
  • 6oik – hAChR M2 (mutant) + guanine nucleotide-binding protein + antibody fragment + transducing b chain 1 – Cryo EM
    
  • 6u1n – hAChR M2/V2R + antibody + arrestin – Cryo EM
    
  • 7t8x, 7t90 – hAChR M2 + guanine nucleotide-binding protein + scFv + acetylcholine – Cryo EM
    
  • 7t94 – hAChR M2 + guanine nucleotide-binding protein + scFv + acetylcholine + modulator + pyridine derivative – Cryo EM
    
  • 1a11 – rAChR M2 transmembrane domain – rat - NMR
    
• Muscarinic acetylcholine receptor M3
  • 8ea0 – hAChR M3 + agonist – Cryo EM
    
  • 8e9y – hAChR M3 + guanine nucleotide-binding protein + scFv + agonist – Cryo EM
    
  • 8e9z – hAChR M3 + guanine nucleotide-binding protein + scFv + agonist + cholesterol – Cryo EM
    
  • 8e9w – hAChR M3 + guanine nucleotide-binding protein + scFv + piperazine derivative – Cryo EM
    
  • 4daj – rAChR M3
    
  • 4u14, 4u15 – rAChR M3 + tiotropium
    
  • 5zhp, 4u16 – rAChR M3 + inhibitor
    
• Muscarinic acetylcholine receptor M4
  • 5dsg – hAChR M4 + tiotropium
    
  • 6kp6 – hAChR M4 (mutant)
    
  • 6d9h, 7ld4 – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + agonist – Cryo EM
    
  • 7ld3 – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + ligand – Cryo EM
    
  • 7v69 – hAChR M4 + guanine nucleotide-binding protein + scFv – Cryo EM
    
  • 7trk – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist – Cryo EM
    
  • 7trs – hAChR M4 + guanine nucleotide-binding protein + scFv + acetylcholine – Cryo EM
    
  • 7trq – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist + modulator – Cryo EM
    
  • 7v6a – hAChR M4 + guanine nucleotide-binding protein + scFv + piperidine derivative – Cryo EM
    
  • 7t96, 7trp – hAChR M4 + guanine nucleotide-binding protein + scFv + acetylcholine + modulator + pyridine derivative – Cryo EM
    
  • 7v68 – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist + modulator + pyridine derivative – Cryo EM
    
  • 8e9x – hAChR M4 (mutant) + guanine nucleotide-binding protein + scFv + agonist – Cryo EM
    
• Muscarinic acetylcholine receptor M5
  • 6ol9 – hAChR M5 + tiotropium