Molecular properties of muscarinic acetylcholine receptors
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- HAGA Tatsuya
- The University of Tokyo
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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.<BR><BR>(Communicated by Masanori OTSUKA, M.J.A.)
収録刊行物
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- Proceedings of the Japan Academy. Ser. B: Physical and Biological Sciences
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Proceedings of the Japan Academy. Ser. B: Physical and Biological Sciences 89 (6), 226-256, 2013
日本学士院
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詳細情報 詳細情報について
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- CRID
- 1390001204144963840
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- NII論文ID
- 130003365120
- 40019673379
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- NII書誌ID
- AA00785485
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- COI
- 1:STN:280:DC%2BC3sjhsVynsA%3D%3D
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- ISSN
- 13492896
- 03862208
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- NDL書誌ID
- 024631182
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- PubMed
- 23759942
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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- PubMed
- CiNii Articles
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- 使用不可