Columbia University

Technology Ventures

Carbonyl erastin derivatives as genotype-specific anticancer agents

Technology #cu14068

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Researchers
Brent Stockwell
Managed By
Beth Kauderer
Patent Protection
US Patent Pending 20160332974

Erastin is a recently identified small molecule with specific antitumor activity that does not harm healthy cells. Erastin targets certain cancers with a specific form of the oncogene RAS, and kills tumor cells through a pathway called ferroptosis. However, conventional erastins lack the stability, selectivity, and potency that make them viable therapeutics for cancer. To address these challenges, this technology is an ensemble of erastin analogs with improved selectivity, potency, and stability compared to conventional erastin. The ensemble initiates cancer cell death through the same ferroptosis pathway, but tolerates a wider variety of RAS mutants and is therefore a more robust treatment. This technology has potential to be used as a collection of genotype-selective anticancer agents.

Erastin analogs with greater stability and potency than conventional erastin with specificity for cancer genotypes

The ensemble of erastin derivatives established in this technology display significantly enhanced stability and potency, resulting in a superior set of anticancer drug candidates. The derivatives also display a keener specificity for certain RAS-type cancers, which improve the protection of healthy cells. Moreover, the use of straightforward chemistry to achieve a significant increase in anti-cancer activity represents an attractive platform to develop inexpensive and effective anti-tumor drugs. The genotype specificity of these erastin derivatives can be used in conjunction with personalized medicine to tailor chemotherapy of RAS-type tumors.

The minor structural modification of erastin results in increased specificity, potency, and stability in in vitro cellular assays when compared to conventional erastin.

Lead Inventor:

Brent Stockwell, Ph.D.

Applications:

  • Pharmaceutical treatment for certain RAS-type tumors
  • Genotype-selective anticancer treatment
  • Potent induction of cell death with minimal damage to healthy cells
  • Tool for researchers investigating the effect of RAS mutations in ferroptosis induction
  • Compound for studying the function of RAS mutants in cancer research

Advantages:

  • Cancer specific
  • Does not harm healthy cells
  • Individual compounds in the ensemble demonstrate genotype specificity to different RAS tumors
  • Increased stability and potency than erastin

Patent Information:

Patent Pending (US 20160332974)

Tech Ventures Reference: IR CU14068

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