Muscarinic acetylcholine receptor

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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 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[1]. mAChRs belong to the family of rhodopsin-like G protein coupled seven transmembrane helix receptors and perform various non-neuronal functions[2]. Disease mAChR M1 agonists are developed for treatment of Alzheimer disease[3]. M2 antagonists are developed for treatment of Alzheimer disease and M3 antagonists for treatment of overactive bladder and chronic obstructive pulmonary disease[4] Structural highlights

3D Structures of muscarinic acetylcholine receptors

Updated on 08-January-2020

References

1. ↑ Ishii M, Kurachi Y. Muscarinic acetylcholine receptors. Curr Pharm Des. 2006;12(28):3573-81. doi: 10.2174/138161206778522056. PMID:17073660 doi:http://dx.doi.org/10.2174/138161206778522056
2. ↑ Ockenga W, Kuhne S, Bocksberger S, Banning A, Tikkanen R. Non-neuronal functions of the m2 muscarinic acetylcholine receptor. Genes (Basel). 2013 Apr 2;4(2):171-97. doi: 10.3390/genes4020171. PMID:24705159 doi:http://dx.doi.org/10.3390/genes4020171
3. ↑ Jiang S, Li Y, Zhang C, Zhao Y, Bu G, Xu H, Zhang YW. M1 muscarinic acetylcholine receptor in Alzheimer's disease. Neurosci Bull. 2014 Apr;30(2):295-307. doi: 10.1007/s12264-013-1406-z. Epub 2014 , Mar 3. PMID:24590577 doi:http://dx.doi.org/10.1007/s12264-013-1406-z
4. ↑ Eglen RM. Muscarinic receptor subtype pharmacology and physiology. Prog Med Chem. 2005;43:105-36. doi: 10.1016/S0079-6468(05)43004-0. PMID:15850824 doi:http://dx.doi.org/10.1016/S0079-6468(05)43004-0