G protein-coupled receptors (GPCRs) serve as the largest family for drug targets for a wide range of indications. Despite their popularity, targeting GPCRs can be very challenging. Drugs can interact with GPCRs to activate a plethora of cellular signaling pathways, many of which the physiological consequences are unclear. For other GPCRs, discovering novel chemical matter has proven very difficult. In the age of machine learning, Biagon is building novel approaches to address challenges with “undruggable” GPCRs and to predict and untangle their signaling complexity. Our approaches are rooted in a combination of biophysics and machine learning to provide powerful solutions for drug developers targeting GPCRs.
Bronzeville - a new approach for GPCR drug discovery
GPCR signaling (or inhibition) is determined by the physical ability of a drug to change the conformational ensemble of the receptor. Biagon’s platform operates on the hypothesis that the equilibrium of the ligand-induced conformational ensemble is linearly proportional to the activation of cellular signals. Bronzeville puts this hypothesis into practice.
Bronzeville-Powered Solutions for GPCR Drug Discovery