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Non-endogenous, constitutively activated known G protein-coupled receptors

  • US 6,806,054 B2
  • Filed: 04/05/2001
  • Issued: 10/19/2004
  • Est. Priority Date: 04/07/2000
  • Status: Expired due to Fees
First Claim
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1. A method for directly identifying a non-endogenous compound as a compound having an activity selected from the group consisting of:

  • inverse agonists, agonists, and partial agonists, to a non-endogenous, constitutively activated version of a known G protein-coupled receptor, said receptor comprising a transmembrane-6 region and an intracellular region, comprising the steps of;

    (a) selecting a non-endogenous version of a known GPCR;

    (b) confirming that the selected non-endogenous GPCR of step (a) is constitutively active;

    (c) contacting a non-endogenous candidate compound with the non-endogenous, constitutively activated GPCR of step of (b); and

    (d) determining, by measurement of the compound efficacy at said contacted receptor, whether said non-endogenous compound is an inverse agonist, an agonist, or a partial agonist to said receptor of step (b);

    wherein said receptor of step (b) comprises the amino acid sequence of SEQ ID NO;

    449.

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