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Literature DB >> 3758027

The reaction site of a non-competitive antagonist in the delta-subunit of the nicotinic acetylcholine receptor.

W Oberthür, P Muhn, H Baumann, F Lottspeich, B Wittmann-Liebold, F Hucho.

Abstract

A site in the primary structure of the nicotinic acetylcholine receptor from Torpedo marmorata covalently labeled with the non-competitive antagonist [3H]triphenylmethylphosphonium (TPMP+) was localized. The label was found in position 262 of the delta-polypeptide chain. This site is specifically labeled in the presence of the agonist carbamoylcholine. Labeling is prevented by the non-competitive antagonist histrionicotoxin. Position 262, probably a serine, is located in the highly conserved membrane-spanning helix M2 (according to the predicted folding scheme of Finer-Moore and Stroud (1984). The relationship of this site to the receptor's ion channel and its regulation is discussed.

Entities: Chemical

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Year: 1986 PMID： 3758027 PMCID： PMC1167045 DOI： 10.1002/j.1460-2075.1986.tb04431.x

Source DB: PubMed Journal: EMBO J ISSN： 0261-4189 Impact factor: 11.598

11 in total

1. Studies on the effect of histrionicotoxin on the monocellular electroplax from Electrophorus electricus and on the binding of (3H)acetylcholine to membrane fragments from Torpedo marmorata.

Authors: G Kato; J P Changeux
Journal: Mol Pharmacol Date: 1976-01 Impact factor: 4.436

2. Role of acetylcholine receptor subunits in gating of the channel.

Authors: B Sakmann; C Methfessel; M Mishina; T Takahashi; T Takai; M Kurasaki; K Fukuda; S Numa
Journal: Nature Date: 1985 Dec 12-18 Impact factor: 49.962

3. Covalent labeling of functional states of the acetylcholine receptor. Effects of antagonists on the receptor conformation.

Authors: A Fahr; L Lauffer; D Schmidt; M P Heyn; F Hucho
Journal: Eur J Biochem Date: 1985-03-15

4. Acetylcholine receptor and ion conductance modulator sites at the murine neuromuscular junction: evidence from specific toxin reactions.

Authors: E X Albuquerque; E A Barnard; T H Chiu; A J Lapa; J O Dolly; S E Jansson; J Daly; B Witkop
Journal: Proc Natl Acad Sci U S A Date: 1973-03 Impact factor: 11.205

5. Cleavage of structural proteins during the assembly of the head of bacteriophage T4.

Authors: U K Laemmli
Journal: Nature Date: 1970-08-15 Impact factor: 49.962

6. Amphipathic analysis and possible formation of the ion channel in an acetylcholine receptor.

Authors: J Finer-Moore; R M Stroud
Journal: Proc Natl Acad Sci U S A Date: 1984-01 Impact factor: 11.205

7. Covalent labeling of the acetylcholine receptor from Torpedo electric tissue with the channel blocker [3H]triphenylmethylphosphonium by ultraviolet irradiation.

Authors: P Muhn; F Hucho
Journal: Biochemistry Date: 1983-01-18 Impact factor: 3.162

8. Primary structures of beta- and delta-subunit precursors of Torpedo californica acetylcholine receptor deduced from cDNA sequences.

Authors: M Noda; H Takahashi; T Tanabe; M Toyosato; S Kikyotani; T Hirose; M Asai; H Takashima; S Inayama; T Miyata; S Numa
Journal: Nature Date: 1983-01-20 Impact factor: 49.962

9. Membranes rich in acetylcholine receptor: characterization and reconstitution to excitable membranes from exogenous lipids.

Authors: W Schiebler; F Hucho
Journal: Eur J Biochem Date: 1978-04

20 in total

Review 6. The nicotinic acetylcholine receptor: the founding father of the pentameric ligand-gated ion channel superfamily.

Authors: Jean-Pierre Changeux
Journal: J Biol Chem Date: 2012-10-04 Impact factor: 5.157

7. GABA-gated chloride channels: regulation, structure and sites of gene expression in the brain.

Authors: H Möhler
Journal: J Protein Chem Date: 1989-06

8. Photoaffinity labeling of functional states of the nicotinic acetylcholine receptor.

Authors: W Oberthür; F Hucho
Journal: J Protein Chem Date: 1988-04

9. The noncompetitive blocker [3H]chlorpromazine labels three amino acids of the acetylcholine receptor gamma subunit: implications for the alpha-helical organization of regions MII and for the structure of the ion channel.

Authors: F Revah; J L Galzi; J Giraudat; P Y Haumont; F Lederer; J P Changeux
Journal: Proc Natl Acad Sci U S A Date: 1990-06 Impact factor: 11.205

10. Galanthamine and non-competitive inhibitor binding to ACh-binding protein: evidence for a binding site on non-alpha-subunit interfaces of heteromeric neuronal nicotinic receptors.

Authors: Scott B Hansen; Palmer Taylor
Journal: J Mol Biol Date: 2007-03-31 Impact factor: 5.469