Peptides as modulators of serpin action

Serpins are key players in the regulation of various physiological functions. In addition, their functional loss owing to genetic variations and polymerization causes severe diseases. It is therefore of interest to target serpins for therapeutic interventions. Increasing knowledge of structure, mechanisms of function and dysfunction, as well as natural modulation of human serpins has opened up new possibilities for structure-guided design of modulators. These might provide the possibility of both inhibition and mimicking of serpin function regarding protease inhibition. Also interference with pathological serpin polymerization might be achievable. Peptides are promising molecules for this purpose since they have been shown to be potent and selective inhibitors of protein-protein interactions. This chapter illustrates how serpin action can be modulated by peptides and how these might be useful for therapeutic intervention.