METHOD OF ASSAYING COMPOUNDS WHICH AFFECT THE ACTIVITY OF G-PROTEIN-COUPLED RECEPTORS BASED ON MEASUREMENT OF RECEPTOR OLIGOMERIZATION

摘要

This invention is a new method of assaying compounds that modulate the activity of Gprotein-coupled receptors based on measurement of changes in the relative proportions of monomericto multimeric receptor polypeptides. More specifically, techniques are described herein whichpermit the prediction of the pharmacological efficacy of drug candidates based solely on theability of the candidate compounds to alter the ratio of receptor monomer to homo-oligomericforms of the receptor. This method provides a novel means of assaying compounds as potentialtherapeutic drugs at G protein-coupled receptors which is greatly simplified and moregenerally applicable than existing methods.