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CHRM1

Official Full Name
cholinergic receptor muscarinic 1
Organism
Homo sapiens
GeneID
1128
Background
The muscarinic cholinergic receptors belong to a larger family of G protein-coupled receptors. The functional diversity of these receptors is defined by the binding of acetylcholine and includes cellular responses such as adenylate cyclase inhibition, phosphoinositide degeneration, and potassium channel mediation. Muscarinic receptors influence many effects of acetylcholine in the central and peripheral nervous system. The muscarinic cholinergic receptor 1 is involved in mediation of vagally-induced bronchoconstriction and in the acid secretion of the gastrointestinal tract. The gene encoding this receptor is localized to 11q13. [provided by RefSeq, Jul 2008]
Synonyms
M1; HM1; M1R;
Bio Chemical Class
GPCR rhodopsin
Protein Sequence
MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVNNYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLISFDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYIQFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSSSERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEVVIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKEKKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYALCNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
Open
Disease
Abdominal pelvic pain, Abnormal micturition, Alzheimer disease, Chronic obstructive pulmonary disease, Corneal disease, Dementia, Dissociative neurological symptom disorder, Dyslipidemia, Dystonic disorder, Epileptic encephalopathy, Frontotemporal dementia, Functional bladder disorder, Gastric ulcer, General pain disorder, Glaucoma, Hyperhidrosis, Indeterminate colitis, Intellectual development disorder, Irritable bowel syndrome, Mild neurocognitive disorder, Neuropathy, Obesity, Parkinsonism, Peptic ulcer, Schizoaffective disorder, Schizophrenia, Sebaceous gland disorder, Solid tumour/cancer
Approved Drug
15 +
Clinical Trial Drug
18 +
Discontinued Drug
15 +

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Detailed Information

Receptors for muscarinic acetylcholine (mAChRs) are members of the broad family of G protein-coupled receptors. Especially in the central nervous system and peripheral nervous system, these receptors are crucial for numerous physiological activities. Mostly showing their binding to acetylcholine, mAChRs exhibit functional variety including physiological reactions like phosphoinositide breakdown, adenylyl cyclase inhibition, and potassium channel mediation. For their regulating functions across many physiological systems, distinct receptor subtypes must be selectively expressed.

Among these, the M1 muscarinic receptor (CHRM1) is a major member of the muscarinic receptor family, distributed extensively in the central nervous system and many peripheral organs, and is engaged in controlling several physiological activities. To assist future targeted treatments conceptually, this paper will provide a thorough analysis of the structure, function, and disease involvement of the CHRM1 gene.

Structure and Function of the CHRM1 Gene

Typical G protein-coupled receptor, the M1 muscarinic receptor is encoded by the CHRM1 gene. Found in the 11q13 area of chromosome 11, this receptor has different expression in several human tissues, most notably in various brain areas including the hippocampal and cerebral cortex.

Cellular-wise, the main purpose of the M1 muscarinic receptor is signal transduction mediated by G proteins. Particularly, activation of the M1 receptor causes potassium channel modulation and phosphoinositide breakdown, therefore affecting cell membrane potential and ion concentration across membranes. Neuronal signal transmission, excitability, and synaptic plasticity all suffer greatly under this method.

Role of M1 Receptor in the Central Nervous System

One of the most important receptors in the central nervous system, the M1 muscarinic receptor is essential for sophisticated brain processes like memory, learning, and cognition as well as for M1 receptors to express themselves most in forebrain areas including the hippocampal, striatum, and cerebral cortex. Research on M1 receptor activation reveals that it stimulates glutamate neurotransmitter release, therefore controlling neural synaptic plasticity—a necessary process for memory building and learning.

Studies show that cognitive deficiencies and neurodegenerative disorders like Alzheimer's disease may be intimately related to the loss or malfunction of M1 receptors. Whereas pharmacological stimulation of M1 receptors may greatly reduce learning and memory deficits, genetic deletion of M1 receptors causes significant losses in cognitive capacities in mouse models. M1 receptors therefore show significant promise for the therapy of neurodegenerative disorders.

Figure 1 shows how epigenetic changes, specifically H3K9me3-induced chromatin condensation, suppress CHRM1 expression, leading to altered acetylcholine response and Ca2+ dynamics, impairing striatal synaptic function in Huntington disease.Figure 1. Epigenetic suppression of CHRM1 and its impact on striatal synaptic function in Huntington's disease. (Lee J, et al., 2013)

Relationship between M1 Receptors and Mental Disorders

Apart from their involvement in cognitive processes, M1 receptors are thought to be crucial in the mechanisms causing mental diseases. Rising research in recent years has shown that the central cholinergic system is essential in the development of mental diseases like schizophrenia and mood disorders, especially stressing the involvement of M1 receptors in the pathogenesis of schizophrenia.

Research on functional abnormalities in M1 receptors has shown that those with schizophrenia may have them in their brains, strongly linked to cognitive deficiencies and hallucinations these people go through. In schizophrenia sufferers, adjusting M1 receptor activation might help with cognitive and psychological problems. Furthermore, attracting scientific attention is the interaction between M1 receptors and mental disorders. Although exploratory research is still underway, evidence points to novel treatment approaches for mood disorders using M1 receptor modulation.

Peripheral Roles of M1 Receptors

Apart from their major role in the central nervous system, M1 receptors' distribution throughout the peripheral nervous system makes them indispensable in many physiological activities. M1 receptors, for example, control gastric acid production and smooth muscle contraction in the gastrointestinal system. M1 receptor activation increases stomach acid output, hence controlling gastrointestinal activities.

M1 receptors control bronchoconstriction brought on by vagus nerve stimulation in the pulmonary system. New therapeutic therapies for reducing symptoms like bronchoconstriction-related breathing problems might result from the modulation of M1 receptors.

CHRM1 Gene and Associated Diseases

Mostly affecting neurodegenerative illnesses and mental disorders, the CHRM1 gene is tightly connected to many other conditions. Functional changes or mutations in the CHRM1 gene might set off disorders like amyotrophic lateral sclerosis (ALS) and frontotemporal dementia.

CHRM1 gene expression is particularly affected in frontotemporal dementia, therefore influencing brain cognitive processes and emotional control. These changes might have a bearing on early illness signs like emotional indifference and memory loss. Concurrently, the function of the CHRM1 gene in ALS has attracted more and more interest because research shows that CHRM1 mutations might be linked with motor neuron degeneration and loss of function.

Moreover, the CHRM1 gene is linked to diseases like overactive bladder, usually marked by symptoms like urine frequency and urgency, maybe resulting from aberrant activation of M1 receptors.

Therapeutic Potential of CHRM1 Targeting Drugs

Given the significant roles CHRM1 plays in various physiological processes, its potential as a drug target is being increasingly explored and applied. Researchers are investigating the possibility of targeting CHRM1 receptors to treat conditions like schizophrenia, Alzheimer's disease, and mood disorders. Selectively activating or inhibiting M1 receptors may help improve cognitive functions and emotional states in patients.

However, strategies for targeting CHRM1 face challenges. Due to the distribution of mAChRs across different tissues and their complex roles in various physiological processes, developing safe and effective drugs requires a deep understanding of receptor characteristics and mechanisms. Moreover, selective regulation of M1 receptors is a key area of current research to avoid non-specific effects on other receptors.

References:

  1. Brannan SK, Sawchak S, et al. Muscarinic Cholinergic Receptor Agonist and Peripheral Antagonist for Schizophrenia. N Engl J Med. 2021 Feb 25;384(8):717-726.
  2. Brown AJH, Bradley SJ, et al. From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease. Cell. 2021 Nov 24;184(24):5886-5901.e22.
  3. Dean B. Muscarinic M1 and M4 receptor agonists for schizophrenia: promising candidates for the therapeutic arsenal. Expert Opin Investig Drugs. 2023;32(12):1113-1121.
  4. Lee J, Hwang YJ, et al. Epigenetic regulation of cholinergic receptor M1 (CHRM1) by histone H3K9me3 impairs Ca(2+) signaling in Huntington's disease. Acta Neuropathol. 2013 May;125(5):727-39.
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