Using structural biology and bioprospecting to design potent inhibitors of kallikrein-related peptidases

Protein proteolysis occupies a pivotal niche in human biology where it controls a plethora of physiological and pathological processes. The goal of the studies in this thesis was to provide novel molecular templates for the design of modulators of proteolytic activity. Three distinct templates were investigated yielding powerful and specific modulators of enzymes with roles in ovarian cancer progression and skin homeostasis. These studies also predicate the utility of these templates in blockade of other proteolytic pathways