[HTML][HTML] Fine tuning muscarinic acetylcholine receptor signaling through allostery and bias
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug
targets for neurological diseases, in particular for Alzheimer's disease and schizophrenia …
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 …
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
Muscarinic acetylcholine receptors (mAChR) play important roles in regulating complex
behaviors such as cognition, movement, and reward, making them ideally situated as …
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 …
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 …
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 …
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 …
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
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 …
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
Benzylquinolone carboxylic acid (BQCA) is the first highly selective positive allosteric
modulator (PAM) for the M 1 muscarinic acetylcholine receptor (mAChR), but it possesses …
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
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 …
(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 …
nucleotide binding protein (G protein)-coupled muscarinic acetylcholine (ACh) receptors …