Results 11 to 20 of about 28,733 (280)

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 López, Peter Keov, David M. Thal, Shailesh N. Mistry, Patrick M. Sexton, J. Robert Lane, Meritxell Canals, Arthur Christopoulos   +8 more
semanticscholar   +11 more sources

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.
Alaa Abdul‐Ridha, J. Robert Lane, Shailesh N. Mistry, Laura López, Patrick M. Sexton, Peter J. Scammells, Arthur Christopoulos, Meritxell Canals   +7 more
semanticscholar   +12 more sources

Flavonoids with M1 Muscarinic Acetylcholine Receptor Binding Activity [PDF]

Molecules, 2014
Muscarinic acetylcholine receptor-active compounds have potential for the treatment of Alzheimer’s disease. In this study, a series of natural and synthetic flavones and flavonols was assayed in vitro for their ability to inhibit radioligand binding at ...
Meyyammai Swaminathan, Chin Fei Chee, Sek Peng Chin, Michael J. C. Buckle, Noorsaadah Abd. Rahman, Stephen W. Doughty, Lip Yong Chung   +6 more
doaj   +4 more sources

Molecular Mechanisms of Bitopic Ligand Engagement with the M1 Muscarinic Acetylcholine Receptor [PDF]

Journal of Biological Chemistry, 2014
Background: Bitopic ligands bind concomitantly to orthosteric and allosteric receptor sites. Results: Residues affecting binding and biased signaling of the selective agonists TBPB and 77-LH-28-1 were identified at the M1 muscarinic receptor. Conclusion:
Peter Keov, Laura López, Shane M. Devine, Céline Valant, J. Robert Lane, Peter J. Scammells, Patrick M. Sexton, Arthur Christopoulos   +7 more
semanticscholar   +5 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.
L. Dwomoh, G. Tejeda, A. Tobin
semanticscholar   +3 more sources

Enhancing remyelination in multiple sclerosis via M1 muscarinic acetylcholine receptor. [PDF]

Mol Pharmacol
Multiple sclerosis (MS) is growing in prevalence; yet, treatments that can reverse the progression of the disease are still needed. One strategy that has shown promise for reversing MS is remyelination by inhibiting the M1 receptor, a member of the muscarinic acetylcholine receptor (mAChR) family.
Chen K, Park E, Abd-Elrahman KS.
europepmc   +4 more sources

Enhanced muscarinic M1 receptor gene expression in the corpus striatum of streptozotocin-induced diabetic rats [PDF]

Journal of Biomedical Science, 2009
Acetylcholine (ACh), the first neurotransmitter to be identified, regulate the activities of central and peripheral functions through interactions with muscarinic receptors. Changes in muscarinic acetylcholine receptor (mAChR) have been implicated in the
Mathew Jobin, Kumar T Peeyush, Gireesh G, Paulose CS   +3 more
doaj   +4 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

Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes [PDF]

Molecular Pharmacology, 2018
The realization of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (mAChR) for the treatment of cognitive decline in Alzheimer’s disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
S. Bradley, Colin Molloy, C. Bundgaard, A. Mogg, K. Thompson, L. Dwomoh, Helen E. Sanger, Michael D. Crabtree, Simon M. Brooke, P. Sexton, C. Felder, A. Christopoulos, L. Broad, A. Tobin, C. Langmead   +14 more
semanticscholar   +3 more sources

Substituted Benzylspiroindolin-2-one Analogues as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1. [PDF]

ACS Med Chem Lett, 2013
Notes The authors declare no competing financial interest. Title: Substituted Benzylspiroindolin-2-one Analogues as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1 Application Number: WO 2013071201A1 Publication date: 16 May ...
Rotella DP.
europepmc   +2 more sources