Method of quantifying the G protein-coupled receptor (GPCR)/G protein coupling using a cell membrane array

摘要

The invention relates to a method for quantifying G protein-coupled receptor (GPCR)-G protein binding by means of using a cell membrane array, which comprises (i) putting an unlabeled candidate compound in contact with a cell membrane array in the presence of labeled GTP or of a labeled, non-hydrolyzable analog thereof, in conditions allowing the interaction between said compound and said GPCR present in said cell membranes, and between said labeled GTP or analog thereof and said G protein present in said membranes; (ii) washing; and (iii) quantifying the signal obtained due to the binding of the labeled GTP (or analog) to said G protein. It is applicable in the analysis of the interaction between compounds and cell membrane receptor proteins and of the intracellular signaling mechanisms triggering this interaction mechanism mediated by said compounds.