A golden age of muscarinic acetylcholine receptor modulation in neurological diseases

AB Tobin - Nature Reviews Drug Discovery, 2024 - nature.com
Over the past 40 years, the muscarinic acetylcholine receptor family, particularly the M1-
receptor and M4-receptor subtypes, have emerged as validated targets for the symptomatic …

ERNEST COST action overview on the (patho) physiology of GPCRs and orphan GPCRs in the nervous system

N Birgül Iyison, C Abboud, D Abboud… - British Journal of …, 2024 - Wiley Online Library
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a
critical role in nervous system function by transmitting signals between cells and their …

M1-selective muscarinic allosteric modulation enhances cognitive flexibility and effective salience in nonhuman primates

SA Hassani, A Neumann, J Russell… - Proceedings of the …, 2023 - National Acad Sciences
Acetylcholine (ACh) in cortical neural circuits mediates how selective attention is sustained
in the presence of distractors and how flexible cognition adjusts to changing task demands …

[HTML][HTML] Potentiation of the muscarinic acetylcholine receptor 1 modulates neurophysiological features in a mouse model of Rett syndrome

HW Dong, K Weiss, K Baugh, MJ Meadows… - …, 2024 - Elsevier
Rett syndrome (RTT) is a neurodevelopmental disorder primarily caused by mutations in the
X chromosome-linked gene Methyl-CpG Binding Protein 2 (MECP2). Restoring MeCP2 …

[HTML][HTML] A M1 muscarinic acetylcholine receptor-specific positive allosteric modulator VU0486846 reduces neurogliosis in female Alzheimer's mice

KS Abd-Elrahman, TLL Colson, S Sarasija… - Biomedicine & …, 2024 - Elsevier
Alzheimer's disease (AD) is the most prevalent type of dementia, disproportionately affecting
females, who make up nearly 60% of diagnosed cases. In AD patients, the accumulation of …

[HTML][HTML] New Light on Prions: Putative Role of PrPc in Pathophysiology of Mood Disorders

AA Chrobak, P Pańczyszyn-Trzewik, P Król… - International Journal of …, 2024 - mdpi.com
Mood disorders are highly prevalent and heterogenous mental illnesses with devastating
rates of mortality and treatment resistance. The molecular basis of those conditions involves …

Discovery of VU6007496: Challenges in the Development of an M1 Positive Allosteric Modulator Backup Candidate

JL Engers, KA Bollinger, RA Capstick… - ACS Chemical …, 2024 - ACS Publications
Herein we report progress toward a backup clinical candidate to the M1 positive allosteric
modulator (PAM) VU319/ACP-319. Scaffold-hopping from the pyrrolo [2, 3-b] pyridine-based …

[PDF][PDF] ERNEST COST action overview on the (patho) physiology of GPCRs and orphan GPCRs in the nervous system

NB Iyison, C Abboud, D Abboud… - British Journal of …, 2024 - researchgate.net
There are> 800 human G protein-coupled receptors (GPCRs). Around half (400) have
sensory functions mediating olfaction, taste, light perception, and pheromone signalling. The …

[HTML][HTML] The Activation of Muscarinic Acetylcholine Receptors Protects against Neuroinflammation in a Mouse Model through Attenuating Microglial Inflammation

K Wang, Y Xie, X Chen, X Ouyang, L Zhao… - International Journal of …, 2024 - mdpi.com
Neuroinflammation is a critical factor that contributes to neurological impairment and is
closely associated with the onset and progression of neurodegenerative diseases. In the …

[HTML][HTML] Muscarinic Receptors and Alzheimer's Disease: New Perspectives and Mechanisms

M Monaco, H Trebesova, M Grilli - Current Issues in Molecular Biology, 2024 - mdpi.com
Alzheimer's disease (AD) is one of the most prevalent neurodegenerative diseases on a
global scale. Historically, this pathology has been linked to cholinergic transmission, and …