Erastin analogs for genotype-selective ferroptosis induction

This technology is an ensemble of modified erastin analogs generated with higher potency, solubility, and stability for pro-ferroptotic activity for tumor cells harboring varying oncogenic RAS^V12 mutations.

Unmet Need: Selective targeting of tumor cells harboring oncogenic RAS mutations

RAS genes are one of the most commonly mutated genes in human cancer, yet their protein products have remained intractable to therapeutic agents. Erastin is a drug that initiates non-apoptotic programmed cell death called ferroptosis, which kills cancer cells and leaves healthy cells intact through selective interactions with oncoprotein RAS^V12. Current therapeutics are being generated with unmodified erastin analogs that are not optimized for the genotype specificity of RAS^V12.

The Technology: Erastin analogs for RAS^V12 genotype specificity

This technology is an ensemble of erastin analogs with an additional ketone moiety, generated for enhanced treatment solubility, stability, and potency for RAS^V12+ tumors. These modified erastin analogs show varying responses depending on the mutational state of RAS^V12, improving the potential for erastin-based genotype-selective treatment strategies.

Applications:

• Therapeutic for RAS^V12+ tumors
• Genotype-selective anticancer treatment
• Potent induction of cell death with minimal damage to healthy cells
• Tool for researchers investigating the effect of RAS^V12 mutations in ferroptosis induction
• Research compound for studying the function of RAS^V12

Advantages:

• Enhanced solubility, stability, and potency of analogs compared to unmodified erastin
• Varying responses depending on RAS^V12 mutational state
• Enhanced genotype specificity
• Similar pro-ferroptotic activity as unmodified erastin

Lead Inventor:

Brent R. Stockwell, Ph.D.

Patent Information:

Patent Issued (US 9,938,245)

Related Publications:

Tech Ventures Reference:

• IR CU14068, CU12324, CU19091

• Licensing Contact: Joan Martinez