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:

Quick Facts:
Tags
AngiogenesisCell growthChemotherapyGliomaHypoxia-inducible factorsNeoplasmPrognosisProteinRadiation therapySmall moleculeTumor suppressor
Inventors
Anna LasorellaAntonio IavaroneDan ShermanEric NiSang Bae LeeTimothy Cardozo
Manager
Kristin Neuman
Departments
Institute for Cancer GeneticsNeurologyPediatrics
Divisions
Columbia University Medical Center (CUMC)
Reference Number
CU17182
Release Date
2023-05-19
Collections
Small MoleculeOncology