About Michael Pollastri
The primary research focus of our lab is on discovery of new therapeutics for neglected tropical diseases, using a "parachute" or "repurposing" approach. In this approach, we identify parasitic targets of importance that have been previously biochemically validated, with a further focus on those targets with human homologs that have been pursued in human drug discovery. We then prepare known ligands previously reported against the human homolog for assessment against the parasite target, and then pursue an optimization program from that starting point. Our first project is focused on trypanosomal phosphodiesterases, enzymes that have ~30% homology to human PDE4 and 5. Other projects focus on trypansomal TOR, Aurora kinases, dihydrofolate reductase, and HDACs. Our secondary area of focus is on chemical technologies. Projects in this category include diversification of lead compounds using reaction screening approaches, applications of flow chemistry, and Green Chemistry.
Medicinal chemistry and Chemical technology
417 Egan Research Center
360 Huntington Ave.
Boston, MA 02115
Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs ...
Chemistry and Chemical Biology Faculty Publications (2012)
In this report we describe our ongoing target repurposing efforts focused on discovery of inhibitors of the essential trypanosomal phosphodiesterase ...
The susceptibility of trypanosomatid pathogens to PI3/mTOR kinase inhibitors ...
Chemistry and Chemical Biology Faculty Publications (2011)
Background Target repurposing utilizes knowledge of "druggable" targets obtained in one organism and exploits this information to pursue new potential ...
Identification and characterization of Kava-derived compounds mediating TNF-α suppression
Chemistry and Chemical Biology Faculty Publications (2009)
There is a substantial unmet need for new classes of drugs that block TNF-α-mediated inflammation, and particularly for small molecule ...