Asset

  • No.

    117

  • Asset Title

    GRK5 - Crucial Regulator in Cardiac Hypertrophy

  • Organization

    Lead Discovery Center

  • Product Type

    Protein

  • Therapeutic Area

    Cardiovascular disease

  • Development Stage

    Hit To Lead or Lead Optimization

  • Technical Summary

    • 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

  • Patent

  • Publication

  • Attachment

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