We develop First-in-Class drugs targeting CXXC5, a negative feedback regulator of the Wnt/beta-catenin pathway, which is overexpressed in tissues of bald, wounded, obese diabetes and NASH patients.
CXXC5 as a target for development of drugs for treatment of these diseases is confirmed by phenotypes for CXXC5 knock out mice and by developing the PTD-DBM peptide interfering CXXC5 binding to Disheveled (Dvl). By topical application, the peptide induced neogenic hair growth and wound healing via activation of Wnt signaling.
With the development of PTD-DBM as a new concept therapeutics for hair-loss and wound, we further screened and characterized small molecules inhibiting CXXC5-Dvl protein-protein interaction (PPI). Mimetics for the hits were newly synthesized, and several candidates are on the way of pre-clinical stage of drug development for treatment of obesity, diabetes, NASH, hair loss and wound healing.
The candidates are specific to the patients who overexpressed CXXC5 without any noticeable abnormalities.