Muscarinic acetylcholine receptors: Novel opportunities for drug development

Andrew C Kruse, Brian Kobilka, Dinesh Gautam, Patrick M Sexton, Arthur Christopoulos, Jurgen Wess

Research output: Contribution to journalArticleResearchpeer-review

244 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)549 - 560
Number of pages12
JournalNature Reviews Drug Discovery
Issue number7
Publication statusPublished - 2014

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