Metabolic diseases targeting by CK Regeon Inc. include obesity, diabetes, and NASH; the diseases overexpressing CXXC5. The orally-applicable small molecular drug candidates recover overall diseases phonotypes including insulin resistance, inflammation, steatosis, liver fibrosis as well as result in long-term glucose controlling effect of diabetes with the improvement of serum parameters including TG, HDL, adiponectin, adipokines, AST/ALT etc.
The drug effects are acquired by restoration of the abnormally suppressed Wnt/beta-catenin signaling target genes including GLP-1, PPARd, WISP1, C/EBPa and PPARa etc. via interference of the CXXC5-Dishevelled (Dvl) protein-protein interaction (PPI).
The topically applicable small molecules and PTD-DBM peptide under-development by CK Regeon Inc. induce neogenic hair growth as well as the re-growth of hair through activation of hair follicular stem cells. The drug candidates including topically applicable PTD-DBM peptide and small molecules function through restoration of the suppressed Wnt/beta-catenin signaling via blockade of CXXC5-Dvl PPI in scalps of the hairless or bald. The Wnt/beta-catenin target genes including Keratin-14, E-cadherin, Collagen, Movo1, Sox1 etc. are expressed by the PTD-DBM or by the small molecule CXXC5-Dvl PPI inhihibitors, and result in hair growth especially neogenic hair growth.
The topically applicable small molecules and PTD-DBM peptide under-development by CK Regeon Inc. enhance wound healing with minimization of scar formation through activation of stem cells reside in skin. By blockade of the CXXC5-Dvl PPI, the drug candidates function through restoration of the suppressed Wnt/beta-catenin signaling and subsequent induction of target genes including VEGF, EGFR, Endothelin1, Collagen, FGF9, PPARd in wounded tissues. The regenerative wound healing effects are attributed by activation of the Wnt/beta-catenin signaling which play roles at multiple stages of the wound healing stages including inflammation, proliferation and remodeling phases.
Short Stature, Osteoporosis
The Wnt/beta-catenin signaling is a well-known pathway involving both longitudinal bone growth and bone mass increment by neogenesis. The orally applicable small molecule drug candidates under development in CK Regeon Inc. increase both length and mass of bone by activation of Wnt/beta-catenin signaling through interference of CXXC5-Dvl PPI. The small molecule-induced activation of the Wnt/beta-catenin pathway enhances longitudinal bone growth around 10% by prolonged-activation of chondrocytes in the growth plates of the teen under going senescence. The bone mineral density also increased by the drug candidates by induction of target genes followed by anagenic bone growth by activation of the Wnt/beta-catenin pathway through the CXXC5-Dvl PPI interference.