Synthesis of non-brain-permeant inhibitor of LZK

National Center For Advancing Translational Sciences

Investigators

Abstract

LZK has been identified as a novel therapeutic target in head and neck cancer. This project aims to synthesize small molecule inhibitors of the LZK kinase that are non-brain permeant to enable proof-of-concept animal studies. During this period, the previously synthesized LZK inhibitors were tested in a PK mouse study, and they all still showed a high brain to plasma ratio. As such, a tolerability screen is now underway to examine whether these inhibitors are indeed toxic to mice. If not, then these compounds can still be used in advanced animal models.