Patent ID: 7294472

Claim:
A method of identifying a GPCR signaling modifying compound that binds to the G Protein binding domain of said GPCR, which comprises: (a) providing a library of candidate compounds to screen for binding to said G protein binding domain of said GPCR; (b) providing a GPCR G protein binding domain binding peptide wherein said GPCR G protein binding domain binding peptide binds to the GPCR with higher affinity than the native G protein peptide; (c) screening said library of candidate compounds for high affinity binding to said G protein binding domain of said GPCR in competition with said GPCR G protein binding domain binding peptide; and (d) determining whether (i) a member of said library of candidate compounds has binding to said G protein binding domain of said GPCR of equal or higher affinity than that of the peptide of step (b) or (ii) a member of said library of candidate compounds results in increased binding affinity of the peptide of step (b) when it binds to said G protein binding domain of said GPCR; and (e) identifying compounds that bind to said G protein binding domain of said GPCR of equal or higher affinity than that of the peptide of step (b) or the binding of which to said G protein binding domain of said GPCR result in increased binding affinity of the peptide of step (b).