Muscarinic acetylcholine receptors: novel opportunities for drug development
By A. Kruse, Brian K. Kobilka, D. Gautam, P. Sexton, Arthur Christopoulos, J. Wess. 2014
393 citations recorded by the source corpus.
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 past few years have witnessed unprecedented new insights into muscarinic receptor physiology, pharmacology and structure. These advances include the first structural views of muscarinic receptors in both inactive and active conformations, as well as a better understanding of the molecular underpinnings of muscarinic receptor regulation by allosteric modulators. These recent findings should facilitate the development of new muscarinic receptor subtype-selective ligands that could prove to be useful for the treatment of many severe pathophysiological conditions.
Subfields: Cellular and Molecular Neuroscience, Molecular Biology
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- Ligand biological activity predicted by cleaning positive and negative chemical correlations (2019, background): “Gene knockout studies suggest that the M1 agonists may ameliorate the symptoms of Alzheimer’s disease and related cognitive disorders as well as ameliorate psychosis-like symptoms in schizophrenia (37, 38).”
- Neuronal activity-dependent control of postnatal neurogenesis and gliogenesis (2018, neutral): “…& Panzanelli 2014, Greger et al. 2017, Iacobucci & Popescu 2017, Yakel 2014) and (b) metabotropic G protein–coupled receptors (GPCRs) with slower kinetics [muscarinic receptor, GABAB, and metabotropic glutamate receptors (mGluRs)] (Kruse et al. 2014, Niswender & Conn 2010, Pin & Bettler 2016).”