Julien Papillon & Thomas Maimone

3:00 p.m. – Opening Remarks

3:05 p.m.  Julien Papillon

Novartis Institutes for BioMedical Research, Cambridge, MA

CYP11B2, the aldosterone synthase, and CYP11B1, the cortisol synthase, are two homologous enzymes implicated in a range of cardiovascular and metabolic diseases. We have previously reported the discovery of LCI699, a dual CYP11B2 and CYP11B1 inhibitor which has provided clinical validation for the lowering of plasma aldosterone as a viable approach to modulating blood pressure in humans, as well as normalizing urinary cortisol in Cushing’s disease patients. This lecture will describe how despite the 93% homology between the two enzymes, highly selective inhibitors could be identified, with pharmaceutical properties suitable for clinical development. Clinical data demonstrating that in vitro selectivity translated into in vivo selectivity in humans will be presented.

4:30 p.m. – Opening Remarks

4:35 p.m.  Thomas Maimone

Department of Chemistry

University of California-Berkeley

The Maimone Research Group

Synthesis of Complex Terpenes from Simple Precursors

Concise total syntheses of biologically active and structurally interesting natural products will be disclosed and the enabling synthetic tactics discussed. Emphasis will be placed on a discussion of complex meroterpene and terpene-derived metabolites. The exploitation of oxidative synthetic processes, as well as methods for complex polycycle synthesis, will be highlighted.