Anti-Cancer Activity of a 2,5-Substituted Pyrimidine

Case ID:
09-947

This technology is a novel class of compounds that induce apoptosis in cancerous cells.

 

Background

ARR molecules (adamantyl-substituted retinoid-related) are a unique class of compounds which have been found to induce apoptosis, or cell death, in a large number of tumor types.  SHP plays a role in cellular proliferation.  Molecules that Interfere with its activity act as tumor suppressors and cause the tumor to die. Recent evidence points to ARR interaction with SHP, and resultant apoptosis.  Indications point to use in inhibiting lung, breast, colorectal, hepatic, ovarian, pancreatic, and prostate cancers, and leukemia.  The invention also induced cell death in a pancreatic cancer stem cell.

              

 

Technology

The inventors have designed and synthesized a unique class of compounds that induce cell death, or apoptosis, in a variety of malignant cells in vitro and in vivo.  The compounds bind to the orphan nuclear receptor small heterodimer partner (SHP) and interfere with its actions of cholesterol synthesis and glucose metabolism.  Treating human malignant cells in tissue culture with the compounds resulted in cell death.  Treating mice, bearing malignant cells, with the compounds resulted in inhibition of tumor growth with minimal toxicity to the mouse.

 

Commercial Applications:

  • Therapeutic for various cancers

 

Stage of Development:

Preclinical; animal and cellular studies performed

 

Competitive Advantages:

  • Can be administered with minimal toxicity

 

Intellectual Property Status:

Patent application filed

 

 

Patent Information:
For Information, Contact:
Joan Dunbar
Associate Vice President for Technology Commercialization
Wayne State University
(313) 577-5542
jcdunbar@med.wayne.edu
Inventors:
Joseph Fontana
Ramzi Mohammad
Lulu Farhana
Amro Aboukameel
Marcia Dawson
Zebin Xia
Keywords:
Analog or Analogue
Anti-cancer