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Natural and engineered kallikrein inhibitors: an emerging pharmacopoeia

Swedberg, Joakim, De Veer, Simon, & Harris, Jonathan (2010) Natural and engineered kallikrein inhibitors: an emerging pharmacopoeia. Biological Chemistry: official scientific journal of the GBM, 391(4), pp. 357-374.

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Abstract

The kallikreins and kallikrein-related peptidases are serine proteases that control a plethora of developmental and homeostatic phenomena, ranging from semen liquefaction to skin desquamation and blood pressure. The diversity of roles played by kallikreins has stimulated considerable interest in these enzymes from the perspective of diagnostics and drug design. Kallikreins already have well-established credentials as targets for therapeutic intervention and there is increasing appreciation of their potential both as biomarkers and as targets for inhibitor design. Here, we explore the current status of naturally occurring kallikrein protease-inhibitor complexes and illustrate how this knowledge can interface with strategies for rational re-engineering of bioscaffolds and design of small-molecule inhibitors.

Impact and interest:

14 citations in Scopus
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15 citations in Web of Science®

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176 since deposited on 13 Jul 2011
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ID Code: 42921
Item Type: Journal Article
Keywords: bioscaffold, drug design, inhibitor, phage display, protease positional scanning synthetic combinatorial library, sunflower trypsin inhibitor
DOI: 10.1515/BC.2010.037
ISSN: 1431-6730
Subjects: Australian and New Zealand Standard Research Classification > BIOLOGICAL SCIENCES (060000) > BIOCHEMISTRY AND CELL BIOLOGY (060100)
Divisions: Current > QUT Faculties and Divisions > Faculty of Health
Current > Institutes > Institute of Health and Biomedical Innovation
Copyright Owner: Copyright 2010 Walter de Gruyter
Copyright Statement: The final publication is available at www.degruyter.com
Deposited On: 13 Jul 2011 23:08
Last Modified: 26 Jul 2013 11:55

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