CONSTITUTIVELY TRANSLOCATING CELL LINE

摘要

PROBLEM TO BE SOLVED: To provide a method for identifying compounds altering internalization of a GPCR (G protein-coupled receptor).

SOLUTION: An agonist-independent method for screening for compounds altering the desensitization of the GPCR is provided. A GRK (G protein-coupled receptor kinase) desensitizing the GPCR in the absence of an agonist and a cell line modifying the GRK are included. The method for identifying whether or not the GPCR is expressed with a plasmic membrane and the GPCR has an affinity for arrestin is provided. Furthermore, a modified GPCR having an increased affinity for the arrestin is included. The modified GPCR is useful for methods for screening for the compounds altering the desensitization comprising the agonist-independent method and the agonist-dependent method described in the specification.

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