Methods for G protein coupled receptor activity screening

Chemistry: analytical and immunological testing – Biospecific ligand binding assay

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435 71, 514 2, G01N 33566, G01N 3353

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active

058829440

ABSTRACT:
A method for screening G protein coupled receptors is provided in which G protein coupled receptors that are constitutively active are determined, such as by measuring receptor phosphorylation agonist independent signalling. When a G protein coupled receptor is found to be regulated by constitutive activity, then assay systems may be set up to classify test compounds as agonists, neutral antagonists, or negative antagonists with respect to G protein coupled receptor signalling and phosphorylation. Such determinations and screening are useful for selecting new pharmaceuticals potentially useful in treating disease states mediated by G protein coupled receptors, with applications including treatments in conjunction with narcotic analgesia.

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