Patent ID: 7332292

Claim:
A method of identifying a compound which alters G protein-coupled receptor (GPCR) internalization, comprising: a) providing a cell comprising a CPCR, an arrestin, and a modified G protein-coupled receptor kinase (GRK) comprising one or more modifications in the amino acid sequence of the four C-terminal amino acids of the GRK as compared to a wild type GRK, wherein said GPCR is at least partially internalized in an agonist-independent manner upon expression of said modified GRK; b) exposing said cell to the compound(s); c) determining the cellular distribution of the GPCR, arrestin, or modified GRK, wherein said modified GRK alters GPCR desensitization in the absence of an agonist as compared to a wild type GRK; and d) monitoring a difference between (1) the distribution of the GPCR, arrestin, or modified GRK in the cell in the presence of the compound(s) and (2) the distribution of the GPCR, arrestin, or modified GRK in the cell in the absence of the compound(s).