Patent ID: 7208279
Filing Date: 2007-04-24
Classification: A61P,C07K,G01N

Abstract:
1. A two-screen method of assaying intracellular G protein coupled receptor (GPCR) signaling inhibition, which comprises: (a) providing a first library comprising peptide members, wherein said library is a biased peptide library and wherein the primary sequences of said members are obtained from a native G protein Gα subunit which consists of SEQ ID NO:38; (b) screening said peptide first library members for binding to said G protein binding domain of said GPCR, wherein said screening comprises a competitive binding assay performed in the presence of a first competitive peptide which consisting of SEQ ID NO:38, to identify high-affinity peptide first library members that bind to said GPCR G protein binding domain with higher affinity than that of said first competitive peptide; (c) selecting a high-affinity peptide first library member identified in (b); (d) providing a second library of member compounds; (e) screening said second library member compounds for binding to said GPCR G protein binding domain, wherein said screening is a competitive binding assay performed in the presence of a second competitive peptide which consists of said selected high affinity peptide first library member of (c), to determine whether a second library member compound binds to said GPCR G protein binding domain with equal or higher affinity than that of said second competitive peptide.