ArticleThe Journal of physiology2001
Aromatics at the murine nicotinic receptor agonist binding site: mutational analysis of the alphaY93 and alphaW149 residues.
Article in The Journal of physiology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 31 citations in OpenAlex.
- Intrasubunit and Intersubunit Steroid Binding Sites Independently and Additively MediateMolecular pharmacology · 2021Article
- Catch-and-hold activation of muscle acetylcholine receptors having transmitter binding site mutations.Biophysical journal · 2014Article
- The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.The Journal of biological chemistry · 2014Article
- The additional ACh binding site at the α4(+)/α4(-) interface of the (α4β2)2α4 nicotinic ACh receptor contributes to desensitization.British journal of pharmacology · 2013Article
- Energy for wild-type acetylcholine receptor channel gating from different choline derivatives.Biophysical journal · 2013Article
- End-plate acetylcholine receptor: structure, mechanism, pharmacology, and disease.Physiological reviews · 2012Review
- Sources of energy for gating by neurotransmitters in acetylcholine receptor channels.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Structure of the pentameric ligand-gated ion channel ELIC cocrystallized with its competitive antagonist acetylcholine.Nature communications · 2012Article
- Functional characterization of the α5(Asn398) variant associated with risk for nicotine dependence in the α3β4α5 nicotinic receptor.Molecular pharmacology · 2011Article
- Additional acetylcholine (ACh) binding site at alpha4/alpha4 interface of (alpha4beta2)2alpha4 nicotinic receptor influences agonist sensitivity.The Journal of biological chemistry · 2011Article
- Glycine hinges with opposing actions at the acetylcholine receptor-channel transmitter binding site.Molecular pharmacology · 2011Article
- Acetylcholine receptor channels activated by a single agonist molecule.Biophysical journal · 2010Article
- Energetics of gating at the apo-acetylcholine receptor transmitter binding site.The Journal of general physiology · 2010Article
- The gating isomerization of neuromuscular acetylcholine receptors.The Journal of physiology · 2010Review
- Long-range coupling in an allosteric receptor revealed by mutant cycle analysis.Biophysical journal · 2009Article
- Unliganded gating of acetylcholine receptor channels.Proceedings of the National Academy of Sciences of the United States of America · 2009Article
- Acetylcholine receptor gating: movement in the alpha-subunit extracellular domain.The Journal of general physiology · 2007Article
- 5-HT3 receptors.Current pharmaceutical design · 2006Review
- Invariant aspartic Acid in muscle nicotinic receptor contributes selectively to the kinetics of agonist binding.The Journal of general physiology · 2004Article
- The role of loop 5 in acetylcholine receptor channel gating.The Journal of general physiology · 2003Article
Corrections and comments
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Authors and funding
1 author at 1 institution in 1 country.
Funding
Abstract
1. Two aromatic residues of the muscle nicotinic receptor putative agonist binding site, a tyrosine in position alpha93 and a tryptophan in position alpha149, were mutated to phenylalanine and the effects of the mutations on receptor properties were investigated using single-channel patch clamp. 2. The alphaY93F mutation reduced the receptor affinity by approximately 4-fold and the channel opening rate constant by 48-fold. The alphaW149F mutation reduced the receptor affinity by approximately 12-fold and the channel opening rate constant by 93-fold. 3. The kinetic properties of hybrid receptors that contained one wild-type and one mutated alpha subunit were also examined. Only one type of hybrid receptor activity was detected. The hybrid receptors had a channel opening rate constant intermediate to those of the wild-type and mutant receptors. It was concluded that the ligand binding sites in the mutated muscle nicotinic receptor contributed equally to channel gating. In the case of the alphaW149F mutation, the presence of the mutation in one of the binding sites had no effect on the binding properties of the other, non-mutated, site. 4. The mutant channel opening and closing rate constants were also estimated in the presence of tetramethylammonium. The data suggested significant interaction between the acetyl group of acetylcholine and the alphaY93 residue.
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