Patent ID: 6518480
Filing Date: 2003-02-11
Classification: A01K,A61K,C07K

Abstract:
A method for eliciting a G protein-coupled response in a eukaryotic cell in vitro, the method comprising the steps of:introducing into a eukaryotic cell in vitro a nucleic acid sequence encoding a modified kappa opioid receptor (KOR) comprising an amino acid sequence selected from the group consisting of amino acids 39-414 of SEQ ID NO:6 and amino acids 39-414 of SEQ ID NO:8, wherein the modified KOR is characterized by: a) an at least 5-fold decreased binding affinity for a selected naturally occurring ligand of a native KOR, b) binding affinity for a synthetic small molecule, and c) G protein-coupled activation of a cellular response upon binding of the synthetic small molecule to the modified KOR, said activation being sufficient to obtain a desired cellular response in the eukaryotic cell, said introducing producing a eukaryotic cell expressing the modified KOR; and contacting the eukaryotic cell expressing the modified KOR with the synthetic small molecule; wherein the synthetic small molecule binds the modified KOR of the eukaryotic cell expressing the modified KOR, thereby activating the modified KOR and inducing the G protein-coupled cellular response activated by the modified KOR.