Methods of identifying negative antagonists for G protein couple

Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...

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435 6, 435 72, 435 8, 435 691, 435325, 435365, 4352523, 43525411, 536 2372, 536 241, 536 231, 530350, G01N 33566, C12N 1539, C12N 510, C07K 1403

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060871156

ABSTRACT:
The present invention is directed to a constitutively active G protein coupled receptor of human herpesvirus 8, as well as a method of identifying negative antagonists of a constitutively active G protein coupled receptor. The method comprises co-expressing in a host cell a constitutively active G protein coupled receptor and a reporter protein, wherein expression of the reporter protein is controlled by a promoter responsive to a signalling pathway activated by the constitutively active G protein coupled receptor; exposing the host cell to a test substance; and determining a level of reporter protein activity, wherein the level of reporter protein activity indicates effectiveness of the test substance as a negative antagonist of the constitutively active G protein coupled receptor. The invention further provides a method of preventing tumor formation or cell proliferation caused by a constitutively active G protein coupled receptor. This method comprises administering an amount of the negative antagonist so identified to a subject in an amount effective to prevent tumor formation or cell proliferation.

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