117
GRK5 - Crucial Regulator in Cardiac Hypertrophy
Lead Discovery Center
Protein
Cardiovascular disease
Hit To Lead or Lead Optimization
• GRK5 is (i) a critical regulator of cardiac GPCR-coupled receptor signaling, (ii) up-regulated in heart failure caused by abnormal hypertrophic stress.
• Stress-induced GRK5 translocation leads to changes in gene expression & irreversible remodeling processes.
• Mouse model: (i) GRK5-KO → prevention of cardiac remodeling processes, (ii) GRK5-OE* → cardiac hypertrophy
• Objective: Prevention of irreversible cardiac remodeling processes (maladaptation) by selective GRK5 blockade
