Dr. Tsantrizos’ program centers on the design and synthesis of molecular tools that can be used to probe biochemical pathways implicated in human diseases. The lab is currently investigating four biological targets: the human 1. farnesyl pyrophosphate synthase (hFPPS), 2. geranylgeranyl pyrophosphate synthase (hGGPPS), 3. metalloproteinase ZMPSTE24, and 4. the HIV-1 reverse transcriptase (RT). Under the large umbrella of each of these projects, the following three objectives summarize the main scope of research efforts: (a) implementation of structure-based screening methods that probe protein/ligand interactions; (b) development of synthetic methodologies amenable to enantioselective synthesis of structurally diverse heterocyclic and peptidomimetic ligands; (c) development of reliable structural and functional assays for guiding structure-activity relationship (SAR) studies. These studies are truly multidisciplinary, involving a seamless integration of synthetic organic chemistry, structural research and biochemistry.