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pubmed-article:19549601pubmed:abstractTextHuman kallikrein-related peptidase 4 (KLK4/prostase), a trypsin-like serine protease, is a potential target for prostate cancer treatment because of its proteolytic ability to activate many tumorigenic and metastatic pathways including the protease activated receptors (PARs). Currently there are no KLK4-specific small-molecule inhibitors available for therapeutic development. Here we re-engineer the naturally occurring sunflower trypsin inhibitor to selectively block the proteolytic activity of KLK4 and prevent stimulation of PAR activity in a cell-based system. The re-engineered inhibitor was designed using a combination of molecular modeling and sparse matrix substrate screening.lld:pubmed
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pubmed-article:19549601pubmed:year2009lld:pubmed
pubmed-article:19549601pubmed:articleTitleSubstrate-guided design of a potent and selective kallikrein-related peptidase inhibitor for kallikrein 4.lld:pubmed
pubmed-article:19549601pubmed:affiliationInstitute of Health and Biomedical Innovation, Queensland University of Technology, Brisbane, Queensland 4059, Australia.lld:pubmed
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pubmed-article:19549601pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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