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RU 1101

Novel Peptide Inhibitors of PRC2 for the Treatment of Cancer

The major challenges in cancer treatment are the overall lack of therapeutic agents, the limited efficacy of the available treatments and the severe side effects due to general cytotoxicity. To overcome these hurdles, current research in cancer biology focuses on elucidating particular disease mechanisms and developing highly specific targeted therapeutic approaches. One new area of cancer research involves understanding the mechanisms associated with epigenetic changes resulting in carcinogenesis, specifically the key enzymes controlling these alterations.

Scientists at the Rockefeller University have recently identified a new mutation that leads to altered activity (reduced methyltransferase activity) of polycomb repressive complex 2 (PRC2), an important developmental regulator of gene expression and key player in tumor progression. This mutation involves a specific amino acid substitution in the genes encoding histone H3 and is highly specific to this activity of PCR2, perhaps by blocking the catalytic site.

Utilizing this valuable mechanistic finding, our scientists have designed peptide inhibitors of PRC2 that can be used as a novel therapeutic agent in the treatment of multiple cancers as well as conditions characterized by faulty PRC2 activity. These new therapeutic peptides would allow for a more targeted cancer treatment, specifically in disease states characterized by mutations of specific histone-encoding genes.

Application

  • Treatment of gliomas such as diffuse intrinsic pontine glioma (DIPG) and supratentorial glioblastoma multiforme (GBMs).
  • Treatment of other cancers characterized by aberrant PRC2 methyltransferase activity such as:
    • leukemia
    • lymphoma
    • breast cancer
    • melanoma
    • bladder cancer
    • gastric cancer
    • endometrial cancer
    • prostate cancer
    • colon cancer
    • Ewing carcinoma
    • non-small cell lung carcinoma

Advantages

Highly specific and targeted approach to treat cancers associated with abnormal PRC2 activity.

Stage of Development

Discovery

Lead Inventors

David Allis

Patent Information and References

For Further Information