Muscarinic Acetylcholine GPCR Assays
Background of Muscarinic Acetylcholine Receptors
Muscarinic acetylcholine receptors (mAChRs) represent a large family of 7-membrane segments that belong to the G-protein coupled receptor family. A total of five subtypes in this family have been discovered, they are named M1 receptor, M2 receptor, M3 receptor, M4 receptor, and M5 receptor, respectively. The mAChRs play an important role in the research of Alzheimer's disease or other neurodegenerative diseases.
Fig.1. Structure of the Muscarinic Acetylcholine receptor 1. (Uniprot ID A0A140LG95; obtained from Alphafold)
Distribution and Function of Muscarinic Acetylcholine Receptors
All five subtypes of mACh receptors are expressed in the central nervous system and the peripheral nervous system, especially in the hippocampus in the brain. The distribution of mACh receptors reflects their function in motor control, attention focus, memory retention, and others.
Subtypes and Mechanisms of Muscarinic Acetylcholine Receptors
M1-M5 receptors bind to acetylcholine (ACh) extracellularly and then interact and activate with G-binding regulatory proteins (G proteins) in the intracellular phase.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
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M1 receptor |
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M2 receptor |
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| M3 receptor | CHRM3 |
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M4 receptor |
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M5 receptor |
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Assay List of Muscarinic Acetylcholine Receptors
Creative Biolabs can provide a range of assays of muscarinic acetylcholine receptors. You can choose the assay in the list or contact us for more information:
Published Data
| Paper Title |
Autophagy induced by Muscarinic Acetylcholine Receptor 1 mediates migration and invasion targeting Atg5 via AMPK/ mTOR pathway in prostate cancer |
| Journal |
Journal of Oncology |
| Published |
2022 |
| Abstract |
Prostate cancer (PCA) is a male malignancy with a high mortality rate, but there is currently no long-term stable and effective cure. The data show that autophagy in prostate cancer provides survival activation for tumor cells under physiological pressure, and affects the sensitivity of radiotherapy and the resistance of PCA chemotherapy drugs. The signaling pathways that lead to autophagy include AMPK, mTOR, MAPK/ERK, and the Beclin1/PI3KIII complex. Previous studies have shown that CHRM1 can promote the proliferation and metastasis of PCA through the Hedgehog pathway, but there is no relevant data reported on the connection between CHRM1 and autophagy. This study focused on CHRM1 and elucidated its role in mediating PCA autophagy, explored possible signal response pathways, and provided a potential solution for PCA. |
| Result |
In this work, researchers quantified the expression of CHRM1 in mice and PCA cell models, and observed the autophagy process of PCA cells by transmission electron microscopy and fluorescent quantitative PCR. In order to explore possible signal response pathways, CHRM1 and Atg5 knockdown models were established, the migration and invasion abilities of CHRM1 and Atg5 knockdown were detected, and the expression of AMPK/mTOR-related target proteins was verified. The data indicated that expression of muscarinic acetylcholine receptor 1 positively regulated PCA cell migration, activation of autophagy, and expression of Atg5. Knockdown experiments showed that the high expression of Atg5 regulated by CHRM1 can contribute to the malignant development of early tumors. The exploration of possible response pathways proved that the AMPK/mTOR pathway is critical for the emergence and progression of autophagy. The experimental results show that muscarinic acetylcholine receptor 1 may target Atg5 in prostate cancer cells through the AMPK/mTOR pathway to induce autophagy-mediated cell migration and invasion, which provides a possible and promising prospect for the research and treatment of PCA.
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Fig.2. CHRM1 expression detect assay. (Wang, 2022)
Reference
- Wang, Q.; et al. Autophagy induced by Muscarinic Acetylcholine Receptor 1 mediates migration and invasion targeting Atg5 via AMPK/ mTOR pathway in prostate cancer. Journal of Oncology. 2022, 1155: 6523195.
