Siragen’s unique drug discovery efforts have been focused on a major molecular enzyme central to both intracellular calcium dyshomeostasis and Tau accumulation. Siragen’s novel target is central to pathways that trigger synaptic dysfunction leading to pathological landmarks of neuro-degenerative disorders. Siragen’s small molecules have been modeled based on intrasteric regulation using a structure-guided design, enhancing drastically the specificity and preventing action on downstream kinases. Inhibiting this target modulates upstream events prior to the onset of pathological changes of Tau hyperphosphorylation, soluble amyloid oligomers, aberrant autophagy, synaptic dysfunction, synapse loss and cell death.
Siragen’s inhibitors are at the lead optimization stage for Alzheimer’s disease. Siragen’s novel drug design platform is also a paradigm shift for creating additional kinase inhibitors. Siragen’s new prototypes of kinase inhibitors can be applicable to a number of diseases in which auto-inhibitory dysfunction is the major mechanism of pathophysiology. At least three classes of diseases have been reported to be causally associated with aberrant kinase activity: central nervous system disorders (depression, schizophrenia), metabolic disorders (obesity and diabetes) and cancers (prostate, liver).