Importance of the membrane in ligand-receptor interactions

NMR data that underscore the importance of the membrane in ligand-receptor interactions were obtained and analyzed. The following hypothesis for acetylcholine (ACh) binding to the acetylcholine receptor (AChR) is proposed: ACh first binds to the membrane, where it adopts its bioactive conformation,...

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Bibliographic Details
Published inBiochemical pharmacology Vol. 40; no. 1; p. 49
Main Authors Behling, R W, Jelinski, L W
Format Journal Article
LanguageEnglish
Published England 01.07.1990
Subjects
Acetylcholine - metabolism
Animals
Binding Sites
Cell Membrane - metabolism
Ligands
Magnetic Resonance Spectroscopy
Molecular Conformation
Receptors, Cholinergic - metabolism
Torpedo
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Summary:NMR data that underscore the importance of the membrane in ligand-receptor interactions were obtained and analyzed. The following hypothesis for acetylcholine (ACh) binding to the acetylcholine receptor (AChR) is proposed: ACh first binds to the membrane, where it adopts its bioactive conformation, and it then rapidly diffuses along the membrane to bind to the AChR in its already-correct conformation. Data used to support this hypothesis include (a) the NMR-determined binding constant of KM = (2.8 +/- 0.6) x 10(3) M-1 for the binding of ACh to the asolectin membrane, (b) the lipid dependence of AChR activity, (c) the location of the ACh binding site close to the membrane surface, and (d) the conformation of ACh in its membrane-bound state. Additional experiments to test this hypothesis are proposed.
ISSN:0006-2952
DOI:10.1016/0006-2952(90)90177-M