Noncompetitive Inhibition of Acetylcholine Receptor

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Information moves from the brain to muscle through neurons. The transfer of information between neuron and muscle involves the release of a chemical called acetylcholine from the neuron and the diffusion of acetylcholine to the muscle. Acetylcholine binds to proteins called acetylcholine receptors on the surface of muscle cells, transiently opening small ion channels in the cell membrane. These channel openings initiate muscle contraction. The electric organs in invertebrates are extraordinarily rich in these acetylcholine receptors and, consequently, are the model system used to study the molecular basis of action of acetylcholine or any other agent that acts on acetylcholine receptors. Over the last twelve years, using quantitative fluorescence spectroscopy, Dr. Johnson has developed a unique approach for the study of structural features of intact ligand receptors. He will continue to use this approach to delineate the sites of binding of inhibitors of the acetylcholine receptor. Specifically, he will localize the sites of binding of two noncompetitive inhibitors of the acetylcholine with respect to the surface and side of the cell membrane, as well as their orientation when bound to the receptor. This information will significantly contribute to the development of a molecular understanding of the actions of chemicals on this receptor. Moreover, concepts and experimental approaches developed in the study of the acetylcholine receptor should easily be exportable to the examination of other neurotransmitter and hormone receptors.