Use of Histone Acetyltransferase Inhibitors as Novel Anti-cancer Therapies

C10974: Anti-Cancer Therapeutic Biomarker

Novelty:

This technology includes a novel histone acetyltransferase (HAT) inhibitor as a therapeutic and biomarker for a vast scope of cancers.

Value Proposition:

Acetylation and deacetylation of histone protein lysine residues are a major mechanism for cellular regulation and are implicated in a wide variety of physiological and disease processes including tumerogenesis. While potent histone deactyltransferases have been discovered with significant clinical impact, the identification of histone acetyltransferase inhibitors has proven to be much more difficult. This technology is the identification of a novel group of potent histone acetyltransferase inhibitors and their downstream effectors, which inhibit tumor cell growth in a broad spectrum of cancers through cell arrest, apoptosis and/or senescence. Other advantages of this invention include:

Technical Details:

Johns Hopkins researchers have identified three histone acetyltransferase inhibitors, C646, C146 and C375, which proved to be competitive at inhibiting p300 versus acetyl-CoA. p300 HAT activity has been shown to mediate critical growth and regulatory pathways in tumor cells. It serves as an important therapeutic target as targeting it can promote cellular responses to DNA damaging agents that are currently ineffective against specific cancers. These novel inhibitors stunt the growth of a wide spectrum of tumor cells and promote cellular senescence. Additionally, these inhibitors have been shown to promote sensitivity to DNA damaging agents, leading to the enhance apoptosis of cancerous cells, after combination with other anti-cancer therapeutics.

Looking for Partners:

To develop and commercialize the technology as novel cancer therapeutic and biomarker.

Stage of Development:

Pre-Clinical

Data Availability:

Animal and in vitro data available

Publications/Associated Cases:

Not available at this time