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Functionalization Of Novel Pp5 Inhibitors, Hope P. Hill

Honors Theses

The overexpression of protein phosphatase 5 has been correlated to tumor cell reproduction making it a candidate for small molecule drug therapy. Selective and potent inhibition of protein phosphatase 2A (PP2A) enzyme has been previously achieved through the development of the molecule fostriecin with key functionality being a lactone and unsaturated linear chain. The large synthetic overhead of fostriecin has led to exploration of other small molecule inhibitors that could mirror fostriecin’s interaction with the active site in the catalytic domain of PP5. The naturally occurring inhibitor, cantharidin, is functionalized with an epoxy containing eleven carbon chain to optimize binding …