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US 6,485,922 B1Granted
Methods for detecting compounds which modulate the activity of an LPA receptor
AssigneeAtairgin Technologies, Inc.
InventorsJames Erickson, J. Graham Goddard, Michael Kiefer
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Abstract
The present invention provides novel methods for identifying and characterizing compounds that modulate the activity of an LPA receptor.
Claims4
A method for detecting compounds of interest which act as inverse agonists of LPA in its interaction with EDG-2, comprising the steps of
- a) exposing a compound and LPA to host fungal cells transgenically expressing the EDG-2 receptor (SEQ ID NO. 20), wherein the EDG-2 receptor is coupled to a response pathway through an interaction with the endogenous G-protein of the host fungal cell, under conditions and for a time sufficient to allow interaction of LPA with the EDG-2 receptor and an associated response through the pathway;
- and
- b) detecting an increase or a decrease in a product of the response pathway resulting from the interaction of the compound with the EDG-2 receptor, relative to the absence of the tested compound, and therefrom determining the presence of an antagonist or an allosteric modulator.
A method for identifying compounds of interest which modulate the activity of EDG-2 receptor comprising the steps of:
- a) contacting recombinant host fungal cells, modified to contain the DNA of SEQ. ID.No.1 which is operably linked to control sequences for expression, wherein the EDG-2 receptor is coupled to a response pathway through an interaction with the endogenous G-protein of the host fungal cell, with at least one compound of interest, and
- b) detecting an increase or a decrease in a product of the response pathway resulting from the interaction of the compound with the EDG-2 receptor, relative to the absence of the compound, wherein the product is a second messenger selected from the group consisting of cAMP, inositol, 1,4,5 triphosphate, Cl− ion, and Ca+2 ion, and therefrom determining the presence of an antagonist or an allosteric modulator.
Dependencies are inferred from the claim text.