Download Specific Inhibitors for Vascular Endothelial Growth Factor Receptors

Specific Inhibitors
for Vascular Endothelial
Growth Factor Receptors
Technology
Doctors Rathinavelu, Pattabiraman, Sridhar, and Dakshanamurthy, through in-silico screening, have identified
a novel class of small molecules, substituted isoindoles, that inhibit vascular endothelial growth factor receptor
(VEGFR inhibitors). In the screening process, the crystal structures of VEGFR1 and VEGFR2 from the protein Data
Bank (PDB) were used for creating the binding models. The receptor structures of the binding models were
energy minimized using the DISCOVER module of INSIGHT II (Accelrys, Biosym Inc., San Diego, CA) and utilized
for docking millions of compounds that were available in the public and the commercially available databases at
Georgetown University. The top-ranked 50 compounds were energy minimized and analyzed further to select the
compounds with anti-tumor activity at the Cancer Biology Laboratory of Nova Southeastern University.
Product
These compounds have anti-tumor activity based upon their anti-angiogenic effects. The inhibition of tumor
growth has been demonstrated in vitro and in vivo. These compounds will be effective against most solid tumors,
but we wish to focus upon breast, prostate, bladder, colorectal, and pancreatic tumors. This product is a low-cost
and safe replacement for drugs like the monoclonal antibody protein drug Avastin.
Patents
A U.S. Patent Application entitled “Vascular Endothelial Receptor Specific Inhibitors” covering the F16 series
of compounds was filed on April 20, 2006. A U.S. Patent Application entitled “Specific Inhibitors for Vascular
Endothelial Growth Factor Receptors” covering the JFD series of compounds was filed on September 21, 2006.
The PCT counterpart was filed on May 8, 2008.
Plan
We are seeking a research collaboration to conduct feasibility studies in our laboratories. This joint product
development effort may result in a small molecule approach to anti-angiogenesis. We wish to participate in
clinical testing as well. The patents are available to option or license.
Contact
Gary S. Margules, Sc.D., Vice President for Research and Technology Transfer
(943) 262-7509
09-147-08RJC