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Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
TLDR
The affinity profiles of several of these antagonists at five cloned human muscarinic receptors stably expressed in Chinese hamster ovary cells are determined. Expand
Molecular basis of receptor/G-protein-coupling selectivity.
  • J. Wess
  • Biology, Medicine
  • Pharmacology & therapeutics
  • 1 December 1998
TLDR
This review provides an overview of recent structural, molecular genetic, biochemical, and biophysical studies that have led to novel insights into the molecular mechanisms governing receptor-mediated G-protein activation and receptor/G-protein coupling selectivity. Expand
Activation and allosteric modulation of a muscarinic acetylcholine receptor
TLDR
The structure of an agonist-bound, active state of the human M2 muscarinic acetylcholine receptor stabilized by a G-protein mimetic camelid antibody fragment isolated by conformational selection using yeast surface display reveals larger conformational changes in the extracellular region and orthosteric binding site than observed in the active states of the β2AR and rhodopsin. Expand
Structure and Dynamics of the M3 Muscarinic Acetylcholine Receptor
TLDR
The structure of the Gq/11-coupled M3 mAChR (‘M3 receptor’, from rat) bound to the bronchodilator drug tiotropium is described and a structural comparison between two members of a mammalian GPCR subfamily displaying different G-protein coupling selectivities is allowed. Expand
Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development
TLDR
Specific mAChR-regulated pathways are identified as potentially novel targets for the treatment of various important disorders including Alzheimer's disease, schizophrenia, pain, obesity and diabetes. Expand
G‐protein‐coupled receptors: molecular mechanisms involved in receptor activation and selectivity of G‐protein recognition
  • J. Wess
  • Chemistry, Medicine
  • FASEB journal : official publication of the…
  • 1 April 1997
TLDR
This review will summarize and attempt to integrate recent data derived from structural, molecular genetic, biochemical, and biophysical studies that have shed new light on the molecular mechanisms involved in receptor activation and selectivity of G‐protein recognition. Expand
Muscarinic acetylcholine receptor knockout mice: novel phenotypes and clinical implications.
  • J. Wess
  • Biology, Medicine
  • Annual review of pharmacology and toxicology
  • 16 January 2004
TLDR
The novel insights gained from gene-targeting techniques to generate mutant mouse strains deficient in each of the five mAChR subtypes should prove instrumental for the development of novel classes of muscarinic drugs. Expand
Molecular biology of muscarinic acetylcholine receptors.
  • J. Wess
  • Chemistry, Medicine
  • Critical reviews in neurobiology
  • 1996
TLDR
Since the mAChRs are typical members of the superfamily of G protein-coupled receptors, the information gathered with this class of receptors should be of broad general relevance. Expand
Multiple Muscarinic Acetylcholine Receptor Subtypes Modulate Striatal Dopamine Release, as Studied with M1–M5 Muscarinic Receptor Knock-Out Mice
TLDR
Results provide unambiguous evidence that multiple mAChR subtypes are involved in the regulation of striatal dopamine release and should contribute to a better understanding of the important functional roles that the muscarinic cholinergic system plays in striatal function. Expand
A chemical-genetic approach to study G protein regulation of β cell function in vivo
TLDR
The findings that conditional and selective activation of β cell Gq/11 signaling in vivo leads to striking increases in both first- and second-phase insulin release, greatly improved glucose tolerance in obese, insulin-resistant mice, and elevated β cell mass, associated with pathway-specific alterations in islet gene expression levels are reported. Expand
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