Georgetown University

Thomas H Walls

Milton L Brown

Mikell Paige

Eliot M Rosen

Simeng Suy

Saijun Fan

Kathryn E Ditmer

Scott Grindrod

Todd Hansen

Radioprotector compounds including 3,3'-diindolylmethane (DIM) analogs, are provided. Further provided are methods for their use in reducing or preventing radiation damage, killing a tumor cell and protecting a non-tumor cell, and treating cancer.

Radioprotector compounds

Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [H]-Batrachotoxin-B ([H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.

Na channels, disease, and related assays and compositions

Growing community of inventors

Arlington, VA, United States of America

Thomas H Walls