Muscarinic acetylcholine receptor
From Proteopedia
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| - | <StructureSection load='5zkb' size='340' side='right' caption='Human muscarinic acetylcholine receptor M2 complex with antagonist (PDB code [[5zkb]])' scene='83/833216/Cv/ | + | <StructureSection load='5zkb' size='340' side='right' caption='Human muscarinic acetylcholine receptor M2 complex with antagonist (PDB code [[5zkb]])' scene='83/833216/Cv/5'> |
== Function == | == 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<ref>PMID:17073660</ref>. mAChRs belong to the family of rhodopsin-like G protein coupled seven transmembrane helix receptors and perform various non-neuronal functions<ref>PMID:24705159</ref>. | + | '''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<ref>PMID:17073660</ref>. mAChRs belong to the family of rhodopsin-like G protein coupled seven transmembrane helix receptors and perform various non-neuronal functions<ref>PMID:24705159</ref>. |
== Disease == | == Disease == | ||
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*[[Receptor]] | *[[Receptor]] | ||
*[[Transmembrane (cell surface) receptors]] | *[[Transmembrane (cell surface) receptors]] | ||
| + | *[[Tiotropium bromide]] | ||
</StructureSection> | </StructureSection> | ||
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**[[6oik]] – hAChR M2 (mutant) + guanine nucleotide-binding protein + antibody fragment + transducing b chain 1 – Cryo EM<br /> | **[[6oik]] – hAChR M2 (mutant) + guanine nucleotide-binding protein + antibody fragment + transducing b chain 1 – Cryo EM<br /> | ||
**[[6u1n]] – hAChR M2/V2R + antibody + arrestin – Cryo EM<br /> | **[[6u1n]] – hAChR M2/V2R + antibody + arrestin – Cryo EM<br /> | ||
| - | **1a11]] – rAChR M2 transmembrane domain – rat - NMR<br /> | + | **[[7t8x]], [[7t90]] – hAChR M2 + guanine nucleotide-binding protein + scFv + acetylcholine – Cryo EM<br /> |
| + | **[[7t94]] – hAChR M2 + guanine nucleotide-binding protein + scFv + acetylcholine + modulator + pyridine derivative – Cryo EM<br /> | ||
| + | **[[1a11]] – rAChR M2 transmembrane domain – rat - NMR<br /> | ||
*Muscarinic acetylcholine receptor M3 | *Muscarinic acetylcholine receptor M3 | ||
| + | **[[8ea0]] – hAChR M3 + agonist – Cryo EM<br /> | ||
| + | **[[8e9y]] – hAChR M3 + guanine nucleotide-binding protein + scFv + agonist – Cryo EM<br /> | ||
| + | **[[8e9z]] – hAChR M3 + guanine nucleotide-binding protein + scFv + agonist + cholesterol – Cryo EM<br /> | ||
| + | **[[8e9w]] – hAChR M3 + guanine nucleotide-binding protein + scFv + piperazine derivative – Cryo EM<br /> | ||
**[[4daj]] – rAChR M3 <br /> | **[[4daj]] – rAChR M3 <br /> | ||
**[[4u14]], [[4u15]] – rAChR M3 + tiotropium<br /> | **[[4u14]], [[4u15]] – rAChR M3 + tiotropium<br /> | ||
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**[[6d9h]], [[7ld4]] – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + agonist – Cryo EM<br /> | **[[6d9h]], [[7ld4]] – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + agonist – Cryo EM<br /> | ||
**[[7ld3]] – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + ligand – Cryo EM<br /> | **[[7ld3]] – hAChR M4/adenosine receptor+ guanine nucleotide-binding protein + ligand – Cryo EM<br /> | ||
| + | **[[7v69]] – hAChR M4 + guanine nucleotide-binding protein + scFv – Cryo EM<br /> | ||
| + | **[[7trk]] – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist – Cryo EM<br /> | ||
| + | **[[7trs]] – hAChR M4 + guanine nucleotide-binding protein + scFv + acetylcholine – Cryo EM<br /> | ||
| + | **[[7trq]] – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist + modulator – Cryo EM<br /> | ||
| + | **[[7v6a]] – hAChR M4 + guanine nucleotide-binding protein + scFv + piperidine derivative – Cryo EM<br /> | ||
| + | **[[7t96]], [[7trp]] – hAChR M4 + guanine nucleotide-binding protein + scFv + acetylcholine + modulator + pyridine derivative – Cryo EM<br /> | ||
| + | **[[7v68]] – hAChR M4 + guanine nucleotide-binding protein + scFv + agonist + modulator + pyridine derivative – Cryo EM<br /> | ||
| + | **[[8e9x]] – hAChR M4 (mutant) + guanine nucleotide-binding protein + scFv + agonist – Cryo EM<br /> | ||
*Muscarinic acetylcholine receptor M5 | *Muscarinic acetylcholine receptor M5 | ||
Current revision
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3D Structures of muscarinic acetylcholine receptors
Updated on 15-July-2024
References
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ Suno R, Lee S, Maeda S, Yasuda S, Yamashita K, Hirata K, Horita S, Tawaramoto MS, Tsujimoto H, Murata T, Kinoshita M, Yamamoto M, Kobilka BK, Vaidehi N, Iwata S, Kobayashi T. Structural insights into the subtype-selective antagonist binding to the M2 muscarinic receptor. Nat Chem Biol. 2018 Dec;14(12):1150-1158. doi: 10.1038/s41589-018-0152-y. Epub, 2018 Nov 12. PMID:30420692 doi:http://dx.doi.org/10.1038/s41589-018-0152-y
