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US 2014/0227718 A1Published application
G protein coupled receptor agonists and antagonists and methods of activating and inhibiting g protein coupled receptors using the same
AssigneeTufts Medical Center, Inc.
InventorsAthan Kuliopulos, Lidija Covic
Life of this patent
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Abstract
The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.
Claims19
1-22. (canceled)
A method for identifying an agent that modulates the activity or function of a G protein coupled receptor (GPCR), the method comprising:
- a. providing a cell comprising said GPCR, or having a property or function ascribable to said GPCR;
- b. contacting said cell with a polypeptide, said polypeptide comprising:
- i. a first domain comprising an intracellular loop, or a fragment thereof, of said GPCR, wherein said fragment comprises at least 3 contiguous amino acid residues of the intracellular loop;
- and
- ii. a second domain, attached to the first domain, wherein said second domain comprises a cell-penetrating, membrane-tethering hydrophobic moiety comprising:
- a lipid, cholesterol, a phospholipid, a steroid, a sphingosine, a ceramide, octyl-glycine, 2-cyclohexylalanine, or benzolylphenylalanine;
- wherein said polypeptide is an agonist or antagonist of said GPCR;
- and
- c. contacting said cell with a candidate agent;
- d. determining whether said candidate agent alters the activity or function of said GPCR;
- wherein, an alternation in the activity or function of said GPCR in the presence of said candidate agent, a as compared to a control in which a cell is not exposed said candidate agent, is indicative that said agent modulates the activity or function of said GPCR.
8 more elements
A method for identifying an agent that modulates the activity or function of a G protein coupled receptor (GPCR), the method comprising:
- a. providing a composition comprising said GPCR in membrane-bound form;
- b. contacting said membrane-bound GPCR with a polypeptide, said polypeptide comprising:
- i. a first domain comprising an intracellular loop, or a fragment thereof, of said GPCR, wherein said fragment comprises at least 3 contiguous amino acid residues of the intracellular loop;
- and
- ii. a second domain, attached to the first domain, wherein said second domain comprises a membrane-tethering hydrophobic moiety comprising:
- a lipid, cholesterol, a phospholipid, a steroid, a sphingosine, a ceramide, octyl-glycine, 2-cyclohexylalanine, or benzolylphenylalanine;
- wherein said polypeptide is an agonist or antagonist of said GPCR;
- and
- c. contacting said membrane-bound GPCR with a candidate agent;
- d. determining whether said candidate agent alters the activity or function of said GPCR;
- wherein, an alternation in the activity or function of said GPCR in the presence of said candidate agent, a as compared to a control in which said GPCR is not exposed said candidate agent, is indicative that said agent modulates the activity or function of said GPCR.
8 more elements
Dependencies are inferred from the claim text.