• Publications
  • Influence
Muscarinic receptor subtypes.
The aim of this review is to discuss the structure, function, and binding properties of the different muscarinic receptor species, attempting where possible to coordinate the diverse experimental data into a uniform picture. Expand
Pirenzepine distinguishes between different subclasses of muscarinic receptors
Binding studies using a new anti-muscarinic drug, pirenzepine, are used, in which heterogeneity of binding is found that correlates well with the pharmacological activity and cannot be taken as evidence for different receptor subtypes. Expand
Ligand binding assays at equilibrium: validation and interpretation
The focus of this review paper is factors affecting data interpretation in ligand binding assays under equilibrium conditions: buffer composition and the temperature at which the assay is conducted, and the impact these can have on affinity measurements and the understanding of drug interactions. Expand
ERKI/II Regulation by the Muscarinic Acetylcholine Receptors in Neurons
It is found that the level of ERKI/II activation in brain is regulated by mAChRs, and the nature of the signal transduction suggests that ERKI-II can serve as a convergence site formAChR activation and other neurotransmitter receptors. Expand
The role of the aspartate-arginine-tyrosine triad in the m1 muscarinic receptor: mutations of aspartate 122 and tyrosine 124 decrease receptor expression but do not abolish signaling.
It is proposed that Asp122 and Tyr124 make intramolecular contacts whose integrity is important for efficient receptor folding but that they do not participate directly in signaling. Expand
Modification of the binding properties of muscarinic receptors by gallamine.
The effects of gallamine on the binding of muscarinic ligand ligands are much greater in heart than in other tissues, suggesting the possibility of developing novel and selective musCarinic drugs. Expand
GPCR activation: a mutagenic spotlight on crystal structures.
  • E. Hulme
  • Biology, Medicine
  • Trends in pharmacological sciences
  • 2013
This review interprets these G-protein-coupled receptor (GPCR) structures through the focus provided by extensive mutagenesis studies on muscarinic receptors, revealing an activation mechanism that is both modular and dynamic. Expand
Alanine-scanning mutagenesis of transmembrane domain 6 of the M(1) muscarinic acetylcholine receptor suggests that Tyr381 plays key roles in receptor function.
A systematic alanine-scanning mutagenesis study on residues Tyr381 to Val387 within the binding domain of the M(1) muscarinic ACh receptor found that the hydroxyl group and benzene ring of Tyr381 both participate in interactions with azanorbornane- and quinuclidine-based ligands and atropine analogs in the ground state as well as the activated state of the receptor. Expand
The binding of agonists to brain muscarinic receptors.
There is quantitative agreement between the agonist affinity constants for the two sites and parameters derived from the action of muscarinic agonists on smooth muscle, and a third (minor) population of "super-high" affinity agonist binding sites has been detected. Expand
Receptor-ligand interactions : a practical approach
Kevin G. McFarthing: Selection and synthesis of receptor-specific radioligands A.D. Strosberg: Anti-receptor antibodies as ligands J.O. Dolly: Neurotoxins as receptor ligands E.C. Hulme & N.J.M.Expand