| abstract |
[PROBLEMS] To inhibit the binding of GRK protein having a PH region or its partial peptide to Gbeta gamma protein, Disclosed is a method for screening for a therapeutic agent for heart failure or a therapeutic agent for hypertension, which can directly confirm inhibition of protein-coupled receptor desensitization. SOLUTION: The screening method of the present invention allows a large amount of compounds to be screened quickly and easily, and the compound obtained by the screening method, which changes the binding between GRK protein and G beta gamma protein, is a therapeutic agent for heart failure, hypertension, etc. Useful as By inhibiting the binding of GRK2 to G beta gamma protein, the phosphorylation of GRK to βAR can be suppressed and its desensitization can be inhibited, so that a drug based on a new mechanism of action can be developed. |