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Negatively charged amino acid residues in the nicotinic receptor delta subunit that contribute to the binding of acetylcholine.
Czajkowski C, Kaufmann C, Karlin A.
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In nicotinic receptors, the binding sites for acetylcholine are likely to contain negatively charged amino acid side chains that interact with the positively charged quaternary ammonium group of acetylcholine and of other potent agonists. We previously found that a 61-residue segment of the delta subunit contains aspartate or glutamate residues within 1 nm of cysteines in the acetylcholine binding site on the alpha subunit. We have now mutated, one at a time, the 12 aspartates and glutamates in this segment of the mouse muscle delta subunit and have expressed the mutant receptors in Xenopus oocytes. Both the concentration of acetylcholine eliciting half-maximal current (Kapp) and the Ki for the inhibition by acetylcholine of alpha-bungarotoxin binding were increased 100-fold by the mutation of delta Asp180 to Asn and 10-fold by the mutation of delta Glu189 to Gln. These two residues, and their homologs in the gamma and epsilon subunits, are likely to contribute to the acetylcholine binding sites.
Abramson,
An analog of lophotoxin reacts covalently with Tyr190 in the alpha-subunit of the nicotinic acetylcholine receptor.
1989, Pubmed
Abramson,
An analog of lophotoxin reacts covalently with Tyr190 in the alpha-subunit of the nicotinic acetylcholine receptor.
1989,
Pubmed Akabas,
Acetylcholine receptor channel structure probed in cysteine-substitution mutants.
1992,
Pubmed
,
Xenbase Baldwin,
Regulation of acetylcholine receptor transcript expression during development in Xenopus laevis.
1988,
Pubmed
,
Xenbase Beeson,
Nucleotide sequence of human muscle acetylcholine receptor beta-subunit.
1989,
Pubmed Blount,
Molecular basis of the two nonequivalent ligand binding sites of the muscle nicotinic acetylcholine receptor.
1989,
Pubmed Blount,
Native folding of an acetylcholine receptor alpha subunit expressed in the absence of other receptor subunits.
1988,
Pubmed Buonanno,
A universal oligonucleotide probe for acetylcholine receptor genes. Selection and sequencing of cDNA clones for the mouse muscle beta subunit.
1986,
Pubmed Camacho,
The epsilon subunit confers fast channel gating on multiple classes of acetylcholine receptors.
1993,
Pubmed
,
Xenbase Charnet,
Structure of the gamma-less nicotinic acetylcholine receptor: learning from omission.
1992,
Pubmed
,
Xenbase Cohen,
Structure of the agonist-binding site of the nicotinic acetylcholine receptor. [3H]acetylcholine mustard identifies residues in the cation-binding subsite.
1991,
Pubmed Criado,
Nucleotide sequence of the rat muscle acetylcholine receptor epsilon-subunit.
1988,
Pubmed Czajkowski,
Agonist binding site of Torpedo electric tissue nicotinic acetylcholine receptor. A negatively charged region of the delta subunit within 0.9 nm of the alpha subunit binding site disulfide.
1991,
Pubmed Damle,
Effects of agonists and antagonists on the reactivity of the binding site disulfide in acetylcholine receptor from Torpedo californica.
1980,
Pubmed Damle,
Affinity labeling of one of two alpha-neurotoxin binding sites in acetylcholine receptor from Torpedo californica.
1978,
Pubmed Dennis,
Amino acids of the Torpedo marmorata acetylcholine receptor alpha subunit labeled by a photoaffinity ligand for the acetylcholine binding site.
1988,
Pubmed Dougherty,
Acetylcholine binding by a synthetic receptor: implications for biological recognition.
1990,
Pubmed Dowding,
Monoclonal antibodies specific for each of the two toxin-binding sites of Torpedo acetylcholine receptor.
1987,
Pubmed Galzi,
Functional significance of aromatic amino acids from three peptide loops of the alpha 7 neuronal nicotinic receptor site investigated by site-directed mutagenesis.
1991,
Pubmed
,
Xenbase Galzi,
Allosteric transitions of the acetylcholine receptor probed at the amino acid level with a photolabile cholinergic ligand.
1991,
Pubmed Galzi,
Identification of a novel amino acid alpha-tyrosine 93 within the cholinergic ligands-binding sites of the acetylcholine receptor by photoaffinity labeling. Additional evidence for a three-loop model of the cholinergic ligands-binding sites.
1990,
Pubmed Glockshuber,
Mapping and modification of an antibody hapten binding site: a site-directed mutagenesis study of McPC603.
1991,
Pubmed Golino,
Subunit requirements for Torpedo AChR channel expression: a specific role for the delta-subunit in voltage-dependent gating.
1992,
Pubmed
,
Xenbase Isenberg,
Nucleotide sequence of the mouse muscle nicotinic acetylcholine receptor alpha subunit.
1986,
Pubmed Kao,
Identification of the alpha subunit half-cystine specifically labeled by an affinity reagent for the acetylcholine receptor binding site.
1984,
Pubmed Kao,
Acetylcholine receptor binding site contains a disulfide cross-link between adjacent half-cystinyl residues.
1986,
Pubmed Karlin,
The arrangement of the subunits of the acetylcholine receptor of Torpedo californica.
1983,
Pubmed KATZ,
A study of the desensitization produced by acetylcholine at the motor end-plate.
1957,
Pubmed Kuipers,
Improved site-directed mutagenesis method using PCR.
1991,
Pubmed Kullberg,
Multiple conductance classes of mouse nicotinic acetylcholine receptors expressed in Xenopus oocytes.
1990,
Pubmed
,
Xenbase Kurosaki,
Functional properties of nicotinic acetylcholine receptor subunits expressed in various combinations.
1987,
Pubmed
,
Xenbase LaPolla,
Isolation and characterization of a cDNA clone for the complete protein coding region of the delta subunit of the mouse acetylcholine receptor.
1984,
Pubmed Lo,
Influence of the gamma subunit and expression system on acetylcholine receptor gating.
1990,
Pubmed
,
Xenbase LOWRY,
Protein measurement with the Folin phenol reagent.
1951,
Pubmed Middleton,
Mapping of the acetylcholine binding site of the nicotinic acetylcholine receptor: [3H]nicotine as an agonist photoaffinity label.
1991,
Pubmed Mishina,
Location of functional regions of acetylcholine receptor alpha-subunit by site-directed mutagenesis.
,
Pubmed
,
Xenbase Mishina,
Molecular distinction between fetal and adult forms of muscle acetylcholine receptor.
,
Pubmed
,
Xenbase Nef,
Structure linkage, and sequence of the two genes encoding the delta and gamma subunits of the nicotinic acetylcholine receptor.
1984,
Pubmed Nelson,
A general method of site-specific mutagenesis using a modification of the Thermus aquaticus polymerase chain reaction.
1989,
Pubmed Neubig,
Equilibrium binding of [3H]tubocurarine and [3H]acetylcholine by Torpedo postsynaptic membranes: stoichiometry and ligand interactions.
1979,
Pubmed Noda,
Structural homology of Torpedo californica acetylcholine receptor subunits.
1983,
Pubmed Numa,
A molecular view of neurotransmitter receptors and ionic channels.
,
Pubmed O'Leary,
Mutational analysis of ligand-induced activation of the Torpedo acetylcholine receptor.
1992,
Pubmed
,
Xenbase Pedersen,
d-Tubocurarine binding sites are located at alpha-gamma and alpha-delta subunit interfaces of the nicotinic acetylcholine receptor.
1990,
Pubmed Pradier,
Use of chemical modifications and site-directed mutagenesis to probe the functional role of thiol groups on the gamma subunit of Torpedo californica acetylcholine receptor.
1989,
Pubmed
,
Xenbase Radić,
Expression of recombinant acetylcholinesterase in a baculovirus system: kinetic properties of glutamate 199 mutants.
1992,
Pubmed Reiter,
Affinity labeling of the acetylcholine receptor in the electroplax: electrophoretic separtion in sodium dodecyl sulfate.
1972,
Pubmed Reynolds,
Molecular weight in detergent solution of acetylcholine receptor from Torpedo californica.
1978,
Pubmed Satow,
Phosphocholine binding immunoglobulin Fab McPC603. An X-ray diffraction study at 2.7 A.
1986,
Pubmed Sine,
Gamma- and delta-subunits regulate the affinity and the cooperativity of ligand binding to the acetylcholine receptor.
1991,
Pubmed Steinbach,
Structural and functional diversity in vertebrate skeletal muscle nicotinic acetylcholine receptors.
1989,
Pubmed Sussman,
Atomic structure of acetylcholinesterase from Torpedo californica: a prototypic acetylcholine-binding protein.
1991,
Pubmed Tomaselli,
Mutations affecting agonist sensitivity of the nicotinic acetylcholine receptor.
1991,
Pubmed
,
Xenbase Yoshii,
Equilibrium properties of mouse-Torpedo acetylcholine receptor hybrids expressed in Xenopus oocytes.
1987,
Pubmed
,
Xenbase Yu,
Mouse muscle nicotinic acetylcholine receptor gamma subunit: cDNA sequence and gene expression.
1986,
Pubmed Yu,
Single-channel properties of mouse-Torpedo acetylcholine receptor hybrids expressed in Xenopus oocytes.
1991,
Pubmed
,
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