The 'nano-environment' of a neurotransmitter receptor

BARRANTES, F.J.

Anales de la Academia Nacional de Ciencias Exactas, Físicas y Naturales de Buenos Aires

ACADEMIA NACIONAL DE CIENCIAS EXACTAS FÍSICAS Y NATURALES

Lugar: Buenos Aires; Año: 2009 vol. 61 p. 55 - 68

0365-1185

The nicotinic acetylcholine receptor (AChR) is the archetype rapid ligand-gated neurotransmitter receptor. It mediates fast intracellular communication in response to the endogenous neurotransmitter acetylcholine, a small organic molecule. Electron-spin resonance spectroscopy has established the stoichiometry and selectivity of the lipid shell surrounding the AChR and disclosed the occurrence of lipid sites. Combined electrophysiological single-channel recordings and site-directed mutagenesis data fostered the identification of such lipid-sensitive residues in the transmembrane region, dissecting their contribution to ligand binding and channel gating, opening and closing. Thus, the interface between the protein moiety and the adjacent lipid shell constitutes the habitat of a variety of pharmacologically relevant processes, including the action of steroids and other lipids.