Screening in Constitutively Active Receptor Systems

Abstract

This unit discusses the use of constitutive G protein‐coupled receptor (GPCR) activity for the screening of new drug entities. It begins with an introduction to constitutive GPCR activity and then centers on the three basic components of a constitutive screening system, namely the receptor, the receptor coupling components (G protein) and the response reporting system. Then, the influence of ligands and particular application of such systems to drug screening, with reference to optimal conditions, is discussed. Finally, the relative advantages and disadvantages of constitutive screening are considered. This unit discusses the use of constitutive G protein‐coupled receptor (GPCR) activity for the screening of new drug entities