S106: Cyanobacterial Natural Products as Starting Points for Drug Discovery

Marine cyanobacteria are rich in bioactive secondary metabolites.  Our chemical investigations have yielded anti-inflammatory and anticancer agents that act on a range of therapeutically relevant targets.  A requisite for their development into therapeutics is the detailed characterization of their mechanisms of action, along with solving the supply problem.  An integrative platform of pharmacological, genomic and proteomic profiling coupled with affinity-based methods assisted us in understanding their activities on the cellular and molecular level.  Total synthesis, structure-activity relationship studies and medicinal chemistry campaigns for prioritized compounds allow us to fine-tune activities and improve selectivity profiles.  Rigorous biological evaluation directed us to specific disease indications and enabled us to perform more targeted preclinical in vitro and in vivo studies.