Asset

  • No.

    104

  • Asset Title

    Novel Apelin Receptor Antagonist

  • Organization

    Cancer Research Horizons

  • Product Type

    Peptide

  • Therapeutic Area

    Oncology

  • Development Stage

    Hit To Lead or Lead Optimization

  • Technical Summary

     Apelin is an endogenous peptide identified as a ligand of the G protein-coupled receptor APJ. Extensive tissue distribution of Apelin and its receptor suggests involvement in many physiological processes, and it has also been shown to participate in pathological processes such as heart failure and cancer. Apelin receptor is over-expressed in a number of cancers including glioblastoma (GBM), cervical, renal, lung and liver cancer. 

     

    • We have developed a lead compound, MM315, which is a potent competitive antagonist of the Apelin receptor, demonstrating a binding affinity of 2.4 nM (pA2=9.55 for cAMP). MM315 shows in vivo efficacy in GBM models, significantly extending survival in intracranial orthotopically implanted mice, and it has potential for synergy with temozolomide and radiation therapy. 

  • Patent

  • Publication

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