Small molecule inhibitors of the ID2/VHL interaction

This technology describes four chemical compounds that are capable of inhibiting the ID2/VHL interaction for downstream inhibition of tumor growth and angiogenesis.

Unmet Need: Inhibitors of the ID2/VHL interaction in tumors

Tumor hypoxia is linked with poor prognosis, malignancy, and treatment resistance. Hypoxia-inducible factor α (HIFα) plays a role in the transcriptional response to hypoxic stress and is highly expressed in tumor cells. In hypoxic conditions, ID2 interacts with von Hippel-Lindau (VHL) tumor suppressor protein and inhibits proteasomal degradation of HIFα, promoting tumor growth, angiogenesis, and cell proliferation.

The Technology: Small molecule inhibitors of the ID2/VHL interaction

The technology presents four chemical compounds that can inhibit the interaction between ID2 and VHL, leading to the degradation of HIFα. These compounds show a dose-dependent response and can achieve a 50-90% inhibition of ID2/VHL interaction. These compounds could be utilized as potential therapeutic agents for treating various cancers, including gliomas, by blocking tumor growth and angiogenesis.

Applications:

• Drug treatment for gliomas and general solid tumors
• Therapeutic for high-grade terminal gliomas
• Drug treatment for vascular diseases involving deregulated angiogenesis
• Research tool for studies of hypoxia and cancer

Advantages:

• Prevention or slowing of tumor growth and angiogenesis
• Degradation of HIFα could increase tumor cells susceptibility to radiotherapy and chemotherapy
• Alternative treatment option for tumors that are resistant to traditional treatment methods

Lead Inventor:

Anna Lasorella, M.D.

Related Publications:

Tech Ventures Reference:

• IR CU17182, CU16166

• Licensing Contact: Kristin Neuman