Scientists Awarded $1.3m to Optimize Chemical Probes to Test an Innovative Approach to Cancer Treatment

Newswise — JUPITER, FL – June 7, 2016 – Scientists from the Florida campus of The Scripps Research Institute (TSRI) have been awarded $1.3 million by the National Cancer Institute of the National Institutes of Health to develop novel compounds to enhance the immune system of patients with cancer. Although not aimed specifically at creating drug candidates, these new chemical tools will be used to explore the role of a large family of proteins that has proven to be a rich source of therapeutic targets.

TSRI’s Professor Patrick R. Griffin and Associate Professor Theodore Kamenecka will be the principal investigators (PIs) of the new three-year collaborative multi-PI grant.

The new study will focus on a protein known as the retinoic acid receptor-related orphan receptors (ROR) gamma and molecules that bind to it (ligands) and activate the receptor (agonists).

"There has been significant interest in the ROR family of proteins because they play key roles in energy and fat metabolism as well as immunity," Griffin said. "Many labs have developed compounds to repress the activity of ROR gamma for use in a range of autoimmune diseases. However, only a few labs, including ours, have described activators of this receptor. This research grant will help us optimize our current set of chemical compounds. These molecules will be used to help trigger immune cells so they will attack and kill tumor cells. The general idea is such compounds will help battle adaptive immune resistance encountered in cancer therapy.”

Mi Ra Chang, senior staff scientist in the Department of Molecular Therapeutics, will lead the development of cancer models for this program.

“Previously we had described a chemical probe that can activate immune cells. This research award will allow us to optimize the potency, selectivity and bioavailability of our ROR gamma agonists,” Kamenecka added. “Optimized probes that have good pharmaceutical properties can then be studied in models of cancer immunotherapy.”

Once that work is completed, the scientists expect to pursue pre-clinical development of the drug candidates.

The number of the grant is R01 CA206493.

About the Scripps Research Institute

The Scripps Research Institute (TSRI) is one of the world's largest independent, not-for-profit organizations focusing on research in the biomedical sciences. TSRI is internationally recognized for its contributions to science and health, including its role in laying the foundation for new treatments for cancer, rheumatoid arthritis, hemophilia, and other diseases. An institution that evolved from the Scripps Metabolic Clinic founded by philanthropist Ellen Browning Scripps in 1924, the institute now employs about 3,000 people on its campuses in La Jolla, CA, and Jupiter, FL, where its renowned scientists—including three Nobel laureates—work toward their next discoveries. The institute's graduate program, which awards PhD degrees in biology and chemistry, ranks among the top ten of its kind in the nation. For more information, see www.scripps.edu/.