Biomedical Engineering Reference
In-Depth Information
Pharmacological Targeting of
Human Tissue Kallikrein-
Related Peptidases
University of Patras, Department of Pharmacy, Rion-Patras, 26500, Greece
9.1.1 Human Tissue Kallikrein-Related Peptidases
Traditionally, proteases were considered as blunt aggressors associated with
protein demolition. As our knowledge on the roles of proteolytic pathways has
largely expanded in recent years, it has become clear that proteases act as highly
specific scissors to process specific protein substrates with various (patho)-
physiological implications. 1 Furthermore, proteolytic systems are organized in
complex cascades that regulate important physiological processes such as food
digestion, complement activation, blood coagulation, etc. 2-4 Activation of an
upstream protease initiates the cascade leading to the serial activation of
downstream zymogens; thus, proteolytic cascades lead to rapid amplification of
the overall proteolytic activity while they provide multiple regulatory points for
fine tuning.
Human kallikreins are serine proteases that are divided into two categories:
the plasma kallikreins and the tissue kallikreins (Figure 9.1A). Plasma kallik-
reins comprise only plasma kallikrein or Fletcher factor (KLKB1) encoded by a
single gene mapped on human chromosome 4q35. This enzyme releases the
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