Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...
Patent
1996-06-11
1998-03-31
Walsh, Stephen
Chemistry: molecular biology and microbiology
Measuring or testing process involving enzymes or...
Involving antigen-antibody binding, specific binding protein...
435325, 4352523, 43525411, G01N 3353, G01N 33566
Patent
active
057337357
ABSTRACT:
A method to determine the site on a receptor or its cognate signaling pathway at which an antagonist acts is disclosed. The method comprises first, (a) determining the effect of an antagonist on a first cell that has been modified to display a mutant form of said receptor. The mutant form constituitively activates the cognate signaling pathway of said receptor. Second, (b) the effect of the antagonist is determined on a second host cell that has been modified to display a tethered form of the receptor. The tethered form is composed of an agonist for said receptor covalently bound thereto whereby said agonist activates the cognate signaling pathway of said receptor. The effect on the cells is determined by measuring the level of an intracellular event that is responsive to the cognate signaling pathway. An antagonist that inhibits the intracellular event in (b) acts at the site of binding for an agonist to the receptor. An antagonist that inhibits the intracellular event in step (a) but not in step (b) acts at an intracellular site associated with the cognate signaling pathway.
REFERENCES:
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Boime Irving
Hsueh Aaron J. W.
Kaufman Claire M.
The Board of Regents of the Leland Stanford Junior University
Walsh Stephen
Washington University
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