Patent ID: 7842470
Filing Date: 2010-11-30
Classification: A61K,A61P,C07K

Abstract:
1. An in vitro assay for identifying a pharmacoperone agent that restores function to a mutant gonadotropin-releasing hormone receptor (GnRHR) protein, comprising: exposing a cell expressing the mutant GnRHR protein to a test agent capable of penetrating a cell membrane; and measuring inositol phosphate (IP) production by the cell, wherein an increase in IP production by the cell expressing the mutant GnRHR protein compared to production of IP by a cell expressing the mutant GnRHR protein not exposed to the test agent indicates that the test agent is a pharmacoperone agent that restores function to the mutant GnRHR, or measuring GnRHR ligand binding and internalization by the cell expressing the mutant GnRHR protein, wherein an increase in GnRHR ligand binding and internalization by the cell expressing the mutant GnRHR protein as compared to GnRHR ligand binding and internalization by the cell expressing the mutant GnRHR protein not exposed to the test agent indicates that the test agent is a pharmacoperone agent that restores function to the mutant GnRHR, wherein the mutant GnRHR protein, prior to exposure to the test agent, does not increase IP production nor increase GnRHR ligand binding and internalization.