[HTML][HTML] Fine tuning muscarinic acetylcholine receptor signaling through allostery and bias

ET Van der Westhuizen, KHC Choy, C Valant… - Frontiers in …, 2021 - frontiersin.org
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug
targets for neurological diseases, in particular for Alzheimer's disease and schizophrenia …

The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation

AM Bender, AT Garrison… - ACS chemical …, 2018 - ACS Publications
The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) was the most recent
mAChR to be cloned and has since emerged as a potential therapeutic target for a number …

Targeting muscarinic acetylcholine receptors for the treatment of psychiatric and neurological disorders

SP Moran, J Maksymetz, PJ Conn - Trends in pharmacological sciences, 2019 - cell.com
Muscarinic acetylcholine receptors (mAChR) play important roles in regulating complex
behaviors such as cognition, movement, and reward, making them ideally situated as …

Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders

GJ Digby, JK Shirey, PJ Conn - Molecular BioSystems, 2010 - pubs.rsc.org
Muscarinic acetylcholine receptors (mAChRs) represent exciting therapeutic targets for the
treatment of multiple CNS disorders. The high degree of conservation of amino acids …

Allosteric modulation of muscarinic acetylcholine receptors

KJ Gregory, PM Sexton… - Current …, 2007 - ingentaconnect.com
Muscarinic acetylcholine receptors (mAChRs) are prototypical Family AG protein coupled-
receptors. The five mAChR subtypes are widespread throughout the periphery and the …

[HTML][HTML] Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation …

V Nawaratne, K Leach, CC Felder, PM Sexton… - Journal of Biological …, 2010 - ASBMB
The recently identified small molecule, 3-amino-5-chloro-6-methoxy-4-methylthieno [2, 3-b]
pyridine-2-carboxylic acid cyclopropylamide (LY2033298), is the first selective allosteric …

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

Z Vuckovic, J Wang, V Pham, JI Mobbs, MJ Belousoff… - Elife, 2023 - elifesciences.org
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug
discovery. Despite decades of research, a molecular-level understanding of the general …

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

A Abdul-Ridha, JR Lane, SN Mistry, L Lopez… - Journal of Biological …, 2014 - ASBMB
Benzylquinolone carboxylic acid (BQCA) is the first highly selective positive allosteric
modulator (PAM) for the M 1 muscarinic acetylcholine receptor (mAChR), but it possesses …

[HTML][HTML] Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor

E Khajehali, C Valant, M Jörg, AB Tobin… - Biochemical …, 2018 - Elsevier
Subtype-selective allosteric modulation of the M 1 muscarinic acetylcholine (ACh) receptor
(M 1 mAChR) is an attractive approach for the treatment of numerous disorders, including …

Regulation of muscarinic acetylcholine receptor signaling

CJ van Koppen, B Kaiser - Pharmacology & therapeutics, 2003 - Elsevier
Multiple mechanisms regulate the signaling of the five members of the family of the guanine
nucleotide binding protein (G protein)-coupled muscarinic acetylcholine (ACh) receptors …