Compound screening based on a window of...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/68 (2006.01) C12Q 1/44 (2006.01) C12Q 1/527 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2135253

A method of testing chemical compounds for their abilities to inhibit chemical-messenger-independent activity of G protein- coupled receptors involving; expressing DNA encoding a G protein- coupled receptor in a cell expression system in such a manner as to generate a reproducible "window of chemical-messenger-independent activity" that allows for discrimination of chemical compounds based on relative ability to inhibit chemical-messenger-independent activity of said G protein-coupled receptor; measuring a quantifiable parameter using biochemical or other assay procedures that indicate the agonist-independent activity of said receptor in said system comprising whole cells or membrane fragments containing G protein, an appropriate effector, and cloned G protein-linked receptor; contacting a test-compound with the system under conditions permitting interaction of the test-compound with said receptor; and measuring the change, if any, of the quantifiable parameter which reflects the ability of the test compound to inhibit the chemical-messenger-independent activity of the G protein-coupled receptor.

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