Method of screening compounds for treating cns disorders
AssigneesSage Therapeutics, Inc., Trustees of Tufts College
InventorsMichael Andrew Ackley, James J. Doherty, Stephen James Moss, Manasa Lakshmi Parakala, Paul A. Davies
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Abstract
Provided herein are screening methods and systems for the identification and evaluation of candidate GABAergic modulators. These candidate agents or compounds are useful for treating or preventing CNS-related disorders.
Claims28
A method of screening for a candidate GABA receptor trafficking modulator comprising the steps of:
- a) contacting a test agent with a cell expressing at least one gamma-aminobutyric acid (GABA) receptor subunit;
- b) measuring a membrane-associated amount of the at least one GABA receptor subunit of the cell;
- c) comparing the membrane-associated amount of the at least one GABA receptor subunit in the cell contacted with the test agent with a membrane-associated amount of the at least one GABA receptor subunit in a cell not contacted with the test agent;
- and
- wherein if the membrane-associated amount in the cell contacted with the test agent is greater than the membrane-associated amount in the cell not contacted with the test agent, the test agent is a candidate GABA receptor trafficking modulator.
(canceled)
A method of screening for a candidate GABA receptor trafficking modulator comprising the steps of:
- a) contacting a test agent with a cell expressing at least one gamma-aminobutyric acid (GABA) receptor subunit;
- b) measuring an expression level of the at least one GABA receptor subunit of the cell;
- c) comparing the expression level of the at least one GABA receptor subunit of the cell contacted with the test agent with an expression level of the at least one GABA receptor subunit of a cell not contacted with the test agent;
- and
- wherein if the expression level of the at least one GABA receptor subunit in the cell contacted with the test agent is greater than the expression level of the at least one GABA receptor subunit in the cell not contacted with the test agent, the test agent is a candidate GABA receptor trafficking modulator.
(canceled)
A method of screening for a candidate GABA receptor trafficking modulator comprising the steps of:
- a) contacting a test agent with a cell expressing at least one gamma-aminobutyric acid (GABA) receptor subunit;
- b) measuring a phosphorylation level of the at least one GABA receptor subunit in the cell contacted with the test agent;
- c) comparing the phosphorylation level of the at least one GABA receptor subunit in the cell contacted with the test agent with a phosphorylation level of the at least one GABA receptor subunit in a cell not contacted with the test agent;
- and
- wherein if the phosphorylation level in the cell contacted with the test agent is greater than the phosphorylation level in the cell not contacted with the test agent, the test agent is a candidate GABA receptor trafficking modulator.
-13. (canceled)
-17. (canceled)
-22. (canceled)
A method of screening for a candidate GABA receptor trafficking modulator comprising the steps of:
- a) contacting a test agent with a cell expressing at least one membrane progesterone receptor (mPR);
- b) measuring an activity level of a mPR signaling pathway in the cell contacted with the test agent;
- c) comparing the activity level of the mPR signaling pathway in the cell contacted with the test agent with an activity level of the mPR signaling pathway in a cell not contacted with the test agent;
- wherein if the activity level of the mPR signaling pathway in the cell contacted with the test agent is greater than the activity level of the mPR signaling pathway in the cell not contacted with the test agent, the test agent is a candidate GABA receptor trafficking modulator.
-28. (canceled)
(canceled)
-40. (canceled)
Dependencies are inferred from the claim text.