Using Nanotechnology to Target Aggressive Cancers

A modified gold nanoparticle is used to target aggressive triple negative breast cancer and melanoma by inhibiting RAD6 which is overexpressed in aggressive and chemoresistant cancers.

Technology Summary

This technology utilizes gold nanoparticles (GNPs) conjugated with a small molecule inhibitor (SMI#9) designed to target RAD6, a protein overexpressed in aggressive and chemoresistant cancer cells. GNPs are preferentially taken up by cancer cells when injected into the blood stream and their safety has been demonstrated in human clinical trials. By blocking RAD6’s ubiquitinating activity, the GNP conjugate inhibits tumor growth and increases the effectiveness of DNA-damaging chemotherapeutics, offering a targeted treatment approach for triple negative breast cancer and melanoma that lack conventional drug delivery markers. The nanoparticle delivery system reduces toxic side effects associated with chemotherapy and improves patient outcomes.

Key Advantages

• Selectively targeting through the DNA repair and canonical Wnt pathways
• Enhances sensitivity to chemotherapy drugs
• Avoids potential for drug resistance response

Market Opportunities

• Lack of effective targeted therapies for cancers without conventional markers
• Limited treatment options for aggressive, chemoresistant cancers like TNBC and melanoma
• Drug resistance caused by RAD6-mediated DNA damage tolerance
• Potential combination treatments to improve platinum drug efficacy
• Non-specific toxicity and side effects of conventional chemotherapy

Stage of Development

Pre-Clinical – in vivo data

Patent Status

Issued 10,588,985

References & Publications

Pharmacological targeting of Rad6 enzyme-mediated translasion synthesis overcomes resistance to platinum-based drugs. J Biol Chem. 2017 Jun 23;292(25):10347-10363

Gold nanoparticle conjugated Rad6 inhibitor induces cell death in triple negative breast cancer cells by inducing mitochondrial dysfunction and PARP-1 hyperactivation: Synthesis and characterization. Nanomedicine. 2016 Apr 12(3):745-57