Allosteric modulators targeting CNS muscarinic receptors

A Bock, R Schrage, K Mohr - Neuropharmacology, 2018 - Elsevier
Muscarinic acetylcholine receptors are G protein-coupled receptors (GPCRs) which are
broadly expressed in the central nervous system (CNS) and other tissues in the periphery …

Allosteric modulators of ligand binding to muscarinic acetylcholine receptors

U Holzgrabe, K Mohr - Drug Discovery Today, 1998 - Elsevier
Allosteric modulators of muscarinic receptors act at a site apart from the common ligand
binding site of the receptor protein. These compounds affect both of the molecular events …

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 …

[HTML][HTML] Functionally selective and biased agonists of muscarinic receptors

A Randáková, J Jakubík - Pharmacological Research, 2021 - Elsevier
Disruption of cholinergic signalling via muscarinic receptors is associated with various
pathologies, like Alzheimer's disease or schizophrenia. Selective muscarinic agonists …

Structure/activity relationships of M 2 muscarinic allosteric modulators

K Mohr, C Tränkle, U Holzgrabe - Receptors and Channels, 2003 - Taylor & Francis
Allosteric modulation of G protein-coupled receptors has been intensively studied at
muscarinic acetylcholine receptors. Findings made with archetypal allosteric agents such as …

[HTML][HTML] Muscarinic acetylcholine receptors: novel opportunities for drug development

AC Kruse, BK Kobilka, D Gautam, PM Sexton… - Nature reviews Drug …, 2014 - nature.com
The muscarinic acetylcholine receptors are a subfamily of G protein-coupled receptors that
regulate numerous fundamental functions of the central and peripheral nervous system. The …

[HTML][HTML] Synthesis and structure–activity relationships of allosteric potentiators of the M4 muscarinic acetylcholine receptor

JP Kennedy, TM Bridges, PR Gentry, JT Brogan… - …, 2009 - ncbi.nlm.nih.gov
The five subtypes of the muscarinic acetylcholine receptor (mAChR1—5 or M1—5) are
differentially expressed G protein-coupled receptors (GPCRs) important to a variety of …

Allosteric modulators and selective agonists of muscarinic receptors

U Holzgrabe, M De Amici… - Journal of Molecular …, 2006 - search.proquest.com
Allosteric modulators of ligand-receptor interactions are found for a variety of receptors
(Christopoulos, 2002). Allosteric agents attach to a binding site being topographically …

[HTML][HTML] Current advances in allosteric modulation of muscarinic receptors

J Jakubik, EE El-Fakahany - Biomolecules, 2020 - mdpi.com
Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated
from the orthosteric binding site for the endogenous neurotransmitter. Allosteric modulators …

Current status of muscarinic M1 and M4 receptors as drug targets for neurodegenerative diseases

CC Felder, PJ Goldsmith, K Jackson, HE Sanger… - …, 2018 - Elsevier
The cholinergic signalling system has been an attractive pathway to seek targets for
modulation of arousal, cognition, and attention which are compromised in …