Patent ID: 7410777

Claim:
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 1B -adrenergic receptor; (b) identifying the endogenous 16 th amino acid residue from the proline residue of step (a), in a carboxy-terminus to amino-terminus direction; (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.