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HDL-like discs for assaying membrane proteins in drug discovery

Fiez-Vandal, Cedric, Leder, Lukas, Freuler, Felix, Sykes, David, Charlton, Steven, Siehler Wagner, Sandra, Schopfer, Ulrich and Duckely, Myriam (2012) HDL-like discs for assaying membrane proteins in drug discovery. Biophysical Chemistry, 165/16. pp. 56-61. ISSN 0301-4622


To broaden the use of the recombinant high-density lipoprotein (rHDL) approach to the characterization of lead compounds, we investigated the pharmacology of the human beta-2-adrenoceptor in nanolipid bilayers (rHDL) with a broad set of beta-adrenoceptor antagonists. To that end, we developed a homogeneous copper-chelate scintillation proximity binding assay (SPA) in order to compare receptor-ligand binding affinities before and after reconstitution into rHDLs. Our results clearly suggest that the receptor in rHDLs display the same pharmacology than in cell membranes and that rHDLs can be used not only to measure affinities for a range of ligands but also to study binding kinetics.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Drug discovery; membrane protein; beta-2-adrenoceptor; G-protein coupled receptor; recombinant high-density lipoprotein; scintillation proximity assay; kinetics
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Date Deposited: 13 Oct 2015 13:14
Last Modified: 13 Oct 2015 13:14