Patent ID: 7410777
Filing Date: 2008-08-12
Classification: A61K,A61P,C07D,C07K,G01N

Abstract:
1. A method for creating a non-endogenous, constitutively active version of an endogenous human G protein coupled receptor (GPCR), said endogenous GPCR comprising a transmembrane 6 region and an intracellular loop 3 region, the method comprising: (a) selecting an endogenous human GPCR comprising a proline residue in the transmembrane-6 region, wherein the GPCR is not the β2-adrenergic receptor or the α (b) identifying the endogenous 16 (c) altering the identified amino acid residue of step (b) to a non-endogenous amino acid residue to create a non-endogenous version of the endogenous human GPCR; and (d) determining if the non-endogenous version of the endogenous human GPCR of step (c) is constitutively active by measuring a difference in an intracellular signal measured for the non-endogenous version as compared with a signal induced by the endogenous human GPCR.