Tech Spotlight: First-In Class GTPase Targeted Cancer Therapeutic & Diagnostic

Dr. Dan Theodorescu, Director of the NCI-designated Comprehensive Cancer Center at the University of Colorado, along with fellow collaborators at the University of Colorado,has identified an effective approach to target the two Ral (Ras-like) GTPase proteins, RalA and RalB, for the treatment of cancer. This research group is also developing a companion diagnostic/prognostic assay that can guide therapy, along with several lead compounds that may constitute a “first-in-class” GTPase targeted cancer therapeutic that does not rely on inhibition of post-translational protein modifications.

Dr. Theodorescu's group has identified several non-proprietary Ral inhibitors as lead candidates for drug derivatization, now the subject of ongoing development aimed at design and synthesis of a novel series of second generation Ral inhibitors with enhanced potency, specificity, and pharmacokinetic properties. Dr. Theodorescu also identified a “transcriptional signature” of 39 genes that respond to depletion of RalA and RalB in vivo, then evaluated the signature in microarray-profiled tumor cohorts. The Ral transcriptional signature score (RTSS) provides a new prognostic tool that can be evaluated and compared alongside current clinical practice, guiding therapy and aggressiveness of treatment.

To read a non-confidential summary of this novel treatment approach, including links to relevant scientific publications, please click the image above. For more CU technologies available for licensing, please visit our Tech Explorer site.