Results 11 to 20 of about 29,353 (245)

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor [PDF]

Journal of Biological Chemistry, 2014
Background: Selective and potent positive allosteric modulators (PAMs) of the M1 mAChR have been recently described. Results: Use of structural analogues and mutagenic mapping identified the mechanistic basis for increased PAM activity.
Abdul-Ridha, Byun, Canals, Christopoulos, Conn, Conn, Dror, Foster, Haga, Hulme, Jones, Katritch, Kenakin, Kennedy, Keov, Kruse, Kruse, Kruse, Kuduk, Kuduk, Kuduk, Lazareno, Leach, Leach, Lebois, Lebon, Ma, Matsui, May, Melancon, Mistry, Motulsky, Nathan, Nawaratne, Nickols, Phillips, Ragnarsson, Shirey, Shonberg, Stevens, Tarr, Valant, Venkatakrishnan   +42 more
core   +8 more sources

Muscarinic acetylcholine receptor M1 mutations causing neurodevelopmental disorder and epilepsy [PDF]

Human Mutation, 2021
De novo rare damaging variants in genes involved in critical developmental pathways, notably regulation of synaptic transmission, have emerged as a frequent cause of neurodevelopmental disorders (NDD).
A. Marcé-Grau, Xabier Elorza-Vidal, Carla Pérez-Rius, Anna Ruiz-Nel Lo, Júlia Sala-Coromina, E. Gabau, R. Estévez, A. Macaya   +7 more
semanticscholar   +6 more sources

Targeting the M1 muscarinic acetylcholine receptor in Alzheimer’s disease [PDF]

Neuronal Signaling, 2022
Alzheimer’s disease (AD) remains a major cause of morbidity and mortality worldwide, and despite extensive research, only a few drugs are available for management of the disease.
Louis Dwomoh, Gonzalo S. Tejeda, A. Tobin   +2 more
semanticscholar   +3 more sources

M1 muscarinic acetylcholine receptor dysfunction in moderate Alzheimer’s disease pathology [PDF]

Brain Communications, 2020
Aggregation of amyloid beta and loss of cholinergic innervation in the brain are predominant components of Alzheimer’s disease pathology and likely underlie cognitive impairment.
J. Yi, Daniel J. Whitcomb, Se Jin Park, Celia Martinez-Perez, S. Barbati, Scott J Mitchell, Kwangwook Cho   +6 more
semanticscholar   +5 more sources

Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor [PDF]

ACS Chemical Neuroscience, 2016
Benzoquinazolinone 1 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR), which is significantly more potent than the prototypical PAM, 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline- 3-carboxylic acid (BQCA). In
Capuano, Ben, Christopoulos, Arthur, Jörg, Manuela, Lane, J Robert, Lane, J. Robert, Lim, Herman, Mistry, Shailesh N, Scammells, Peter J, Scammells, Peter J.   +8 more
core   +3 more sources

Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes [PDF]

Science, 2019
Choosing a partner G protein–coupled receptors (GPCRs) bind ligands outside the cell and trigger events inside the cell by selectively binding and activating specific G proteins. The selectivity occurs even among highly related GPCRs.
S. Maeda, Q. Qu, M. J. Robertson, G. Skiniotis, B. Kobilka   +4 more
semanticscholar   +3 more sources

Molecular Determinants of Allosteric Modulation at the M1 Muscarinic Acetylcholine Receptor* [PDF]

Journal of Biological Chemistry, 2014
Background: BQCA is a selective allosteric modulator of the M1 mAChR. Results: Residues that govern BQCA activity were identified using mutagenesis and molecular modeling.
Alaa Abdul-Ridha, Laura Lopez, Peter Keov, D. Thal, Shailesh N Mistry, P. Sexton, J. R. Lane, Meritxell Canals, A. Christopoulos   +8 more
semanticscholar   +6 more sources

Muscarinic Acetylcholine Receptor M1 [PDF]

Definitions, 2020

semanticscholar   +2 more sources

Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias

Frontiers in Pharmacology, 2021
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen, K. H. Christopher Choy, Celine Valant, Simon McKenzie-Nickson, Sophie J. Bradley, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos   +7 more
doaj   +2 more sources

Allosteric Modulation of M1 Muscarinic Acetylcholine Receptor Internalization and Subcellular Trafficking* [PDF]

Journal of Biological Chemistry, 2014
Background: The effects of allosteric modulators on G protein-coupled receptor trafficking are largely unknown. Results: The allosteric ligand BQCA modulates M1 mAChR arrestin recruitment and receptor trafficking.
Holly R. Yeatman, J. R. Lane, K. H. C. Choy, N. Lambert, P. Sexton, A. Christopoulos, Meritxell Canals   +6 more
semanticscholar   +3 more sources