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 theactivity of G protein-coupled receptors based on measurement of changes in therelative proportions of monomeric to multimeric receptor polypeptides. Morespecifically, techniques are described herein which permit the prediction ofthe pharmacological efficacy of drug candidates based solely on the ability ofthe candidate compounds to alter the ratio of receptor monomer to homo-oligomeric forms of the receptor. This method provides a novel means ofassaying compounds as potential therapeutic drugs at G protein-coupledreceptors which is greatly simplified and more generally applicable thanexisting methods.