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Unleashing the therapeutic potential of human kallikrein-related serine proteases

Published on Mar 1, 2015in Nature Reviews Drug Discovery57.618
· DOI :10.1038/nrd4534
Ioannis Prassas14
Estimated H-index: 14
,
Azza Eissa5
Estimated H-index: 5
+ 1 AuthorsEleftherios P. Diamandis99
Estimated H-index: 99
Abstract
Members of the family of kallikrein (KLK)-related proteases are found in various tissues — including the airway, prostate and brain — and have a wide range of functions. The authors describe the roles of KLKs in health and disease, and highlight the small-molecule, peptide-based, protein-based, antibody-based and immunotherapeutic strategies that are being used to target KLKs in certain diseases.
  • References (229)
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Prostate-specific antigen (PSA or kallikrein-related peptidase-3, KLK3) exerts chymotrypsin-like proteolytic activity. The main biological function of PSA is the liquefaction of the clot formed after ejaculation by cleavage of semenogelins I and II in seminal fluid. PSA also cleaves several other substrates, which may explain its putative functions in prostate cancer and its antiangiogenic activity. We compared the proteolytic efficiency of PSA towards several protein and peptide substrates and ...
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