Method for improving the function of heterologous G protein-coupled receptors
AssigneesBASF SE, The United States of America as represented by the Department of Health
InventorsMark Henry Pausch, Jurgen Wess
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Abstract
This invention relates to mutant G protein-coupled receptors with improved G-protein coupling and receptor response, yeast cells expressing such receptors, vectors useful for making such cells, and methods of making and using same.
Claims11
A yeast cell comprising a nucleic acid sequence encoding a mutated, heterologous G protein-coupled receptor, wherein the mutation is a deletion mutation in (1) the 3rd intracellular loop resulting in a 44 amino acid third intracellular loop comprising 22 residues proximal to the 5th and the 6th transmembrane domains or (2) the C-terminus, said mutation improving the function of said heterologous G protein-coupled receptor by causing it to couple more efficiently with a heterotrimeric G protein compared to a wild-type form of the heterologous G protein-coupled receptor, and wherein the mutated G protein-coupled receptor is selected from the group consisting of a muscarinic acetylcholine receptor, a cholecystokinin CCKB receptor, a somatostatin receptor, and a serotonin receptor.
A yeast cell comprising a heterologous G protein-coupled receptor, wherein the G protein-coupled receptor has a deletion in the 3rd intracellular loop resulting in a 44 amino acid third intracellular loop comprising 22 residues proximal to the 5th and the 6th transmembrane domains, said deletion improving the function of said heterologous G protein-coupled receptor by causing it to couple more efficiently with a heterotrimeric G protein as compared to a wild-type form of the heterologous G protein-coupled receptor.
Dependencies are inferred from the claim text.