Cristian G. Bologa, Ph.D.
Research Professor, Department of Internal Medicine, Division of Translational Informatics
Health Sciences Center
The University of New Mexico
Dr. Bologa has disclosed seven inventions to STC, received two UNM-affiliated issued U. S. patents, has one pending U. S. patent application, and a license agreement with Sandia Biotech, Inc. for his estrogen receptor technologies.
Dr. Bologa’s estrogen receptor technology is a class of compounds that specifically bind to estrogen receptors alpha/beta and GPR30 for use in treating diseases and conditions that are regulated by these receptors. Because estrogens, a group of steroid compounds or hormones, are involved in almost every aspect of human physiology and play a critical role in many diseases, G-protein-coupled receptors (GPCRs) are the targets of nearly half the prescription drugs on the market. The compounds are promising candidates for drug development and treatment of many diseases and conditions such as cancer and cardiovascular, inflammatory, neurodegenerative diseases.
Fructose consumption has increased by almost 50 percent among U. S. adults in the last 30 years and is linked to high blood pressure, obesity, diabetes and cancer. Fructose is transported across various cell membranes by members of the facilitated glucose transporter family of proteins called GLUTs. GLUT5 is fructose specific, and is expressed in the intestine, sperm, brain, fat, skeletal muscle and kidney cells. GLUT5 is linked with various pathologies including an overexpression rate in cancer cells, meaning GLUT5 can be used as a marker for cancer. Currently, there are no known inhibitors of GLUT5 that do not interfere with the transport of glucose, which is the human body’s source of fuel.
Dr. Bologa’s GLUT5 inhibitor technology does not affect the glucose transport activity of other GLUTs. The inhibitor is over 3 orders of magnitude more potent on GLUT5 compared to fructose, and achieves complete blockade of GLUT5-mediated fructose transport, with no effect on transporters GLUT1, GLUT2, GLUT3 and GLUT4. The inhibitor could serve as a chemical probe to explore novel therapeutic approaches to treating obesity, diabetes and cancer. Additionally, the inhibitor is not toxic to cells and could promote new research centered around designing GLUT5-specific compounds.
Dr. Bologa’s research focuses on cheminformatics, small-molecule and protein modeling, and ligand- and structure-based virtual screening for molecular discovery. Dr. Bologa designed and performed the virtual screen and selected for testing the compounds that ultimately led to the discovery of the very potent and selective agonist G-1 for the membrane estrogen receptor GPR30.
ISSUED U. S. PATENTS (UNM-AFFILIATED)
7,875,721 Compounds for Binding to ER alpha/beta and GPR30, Methods of Treating Disease States and Conditions Mediated Through These Receptors and Identification Thereof, issued January 25, 2011
8,487,100 Compounds for Binding to ER Alpha/Beta and GPR30, Methods of Treating Disease States and Conditions Mediated through these Receptors and Identification Thereof, issued July 16, 2013
PENDING U. S. PATENT APPLICATIONS
Human GLUT5 Specific Inhibitors and Methods of Treatment