Asset

  • No.

    109

  • Asset Title

    Small Molecule for Treatment-Resistant Lung Cancer

  • Organization

    Emory University

  • Product Type

    Small molecule

  • Therapeutic Area

    Oncology

  • Development Stage

    Hit To Lead or Lead Optimization

  • Technical Summary

    • KRA-533 activates KRAS by preventing the cleavage of GTP into GDP, leading to the accumulation of GTP-KRAS, an active form of KRAS. Treatment of human lung cancer cells with KRA-533 resulted in increased KRAS activity and suppression of cell growth. 

    • Lung cancer patients with KRAS mutation(s) have a poor prognosis due in part to the development of resistance to currently available therapeutic interventions. Currently, there are no effective targeted therapies for patients with the KRAS mutation. 

    • Overcoming these hurdles, Emory researchers have identified a small molecule KRAS agonist that specifically binds the protein and induces cell death in mutant KRAS lung cancer cells. Lung cancer cell lines with KRAS mutation were relatively more sensitive to the small molecule than cell lines without KRAS mutation. Additionally, this molecule suppresses malignant growth without significant toxicity to normal tissues. 

  • Patent

    US20210137953A1

  • Publication

    Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy. Molecular Cancer (2019)

  • Attachment

TOP