The Du Bois Laboratory is leveraging the power of molecular design and chemical synthesis to address problems in catalysis, natural product assembly, chemical biology, and pharmacology. An outstanding goal of our program has been to develop C–H bond oxidative processes as general methods for organic synthesis and to demonstrate the utility of such tools in synthetic planning. These methods continue to be exploited for the purpose of preparing polyfunctionalized carbo- and heterocyclic structures. A second program of interest focuses on the role of ion channels in electrical conduction and the specific involvement of such proteins in the sensation of pain. De novo chemical synthesis of naturally occurring small molecule toxins in combination with the tools of molecular biology, electrophysiology, and cellular imaging enable the interrogation of mechanisms associated with ion channel expression, membrane translocation, turnover, and conduction.