TAILIEUCHUNG - Báo cáo khoa học: The lipid ⁄ protein interface as xenobiotic target site Kinetic analysis of tadpole narcosis

High-resolution X-ray diffraction structures of integral membrane proteins have revealed various binding modes of lipids, but current spectroscopic studies still use uniform macroscopic binding constants to describe lipid binding. The Adair approach employing microscopic lipid-binding con-stants has previously been taken to explain the enhancement of agonist binding to the nicotinic acetylcholine receptor by general anaesthetics in terms of the competitive displacement of essential lipid activator molecules [Walcher S, Altschuh J & Sandermann H (2001) J. Biol. Chem. 276, 42191–42195] | ềFEBS Journal The lipid protein interface as xenobiotic target site Kinetic analysis of tadpole narcosis Joachim Altschuh1 Sebastian Walcher2 and Heinrich Sandermann Jr3 4 1 Institute of Biomathematics and Biometry GSF - NationalResearch Center for Environment and Health Neuherberg Germany 2 LehrstuhlA fur Mathematik RWTH Aachen Germany 3 Institute of BiochemicalPlant Pathology GSF - NationalResearch Center for Environment and Health Neuherberg Germany 4 Germany Keywords Adair theory kinetic modelling lipid protein interface nicotinic acetylcholine receptor tadpole narcosis Correspondence H. Sandermann GSF - NationalResearch Center for Environment and Health Institute of BiochemicalPlant Pathology Ingolstadter LandstraBe 1 D-85764 Neuherberg Germany Fax 49 89 3187 3383 Tel 49 89 3187 2285 E-mail sandermann@ Received 16 December 2004 revised 4 March 2005 accepted 10 March 2005 High-resolution X-ray diffraction structures of integral membrane proteins have revealed various binding modes of lipids but current spectroscopic studies still use uniform macroscopic binding constants to describe lipid binding. The Adair approach employing microscopic lipid-binding constants has previously been taken to explain the enhancement of agonist binding to the nicotinic acetylcholine receptor by general anaesthetics in terms of the competitive displacement of essential lipid activator molecules Walcher S Altschuh J Sandermann H 2001 J. Biol. Chem. 276 42191-42195 . This approach was extended to tadpole narcosis induced by alcohols. A single class or two different classes of lipid activator binding sites are considered. Microscopic lipid and inhibitor binding constants are derived and allow a close fit to dose-response curves of tadpole narcosis on the basis of a preferential displacement of more loosely bound essential lipid activator molecules. This study illustrates the potential of the Adair approach to resolve protein-bound lipid populations. doi .

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