Purdue Institute for Drug Discovery

GRK2 Inhibitors

Overview: 

A set of small molecules based upon a paroxetine to selectively inhibit G Protein-Coupled Receptor Kinase 2 (GRK2) for the treatment of heart failure.

 

Status: 

Purdue Faculty: 

Dr. John Tesmer

Research Articles: 

Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors

Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine