Abstract
Kallikrein-related peptidase-3 (KLK3, known also as prostate-specific antigen, PSA) is highly expressed in the prostate. KLK3 possess antiangiogenic activity, which we have found to be related to its proteolytic activity. Thus, it may be possible to slow down the growth of prostatic tumors by enhancing this activity. We have developed peptides that enhance the proteolytic activity of KLK3. As these peptides are degraded in circulation and rapidly excreted, we have started to modify them and have succeeded in creating bioactive and more stable pseudopeptides. We have also identified small molecules stimulating the activity of KLK3, especially in synergy with peptides.
Acknowledgments
Our original studies reviewed in this paper have been supported by grants from the Helsinki University Central Hospital, the Finnish Cancer Foundation, the Academy of Finland, Sigrid Jusélius Foundation, Graduate School of Organic Chemistry and Chemical Biology, the Research Funds of the University of Helsinki, Finska Läkaresällskapet, Finnish Funding Agency for Technology and Innovation, Magnus Ehrnrooth Foundation, the Swedish Research Council and Biomedicum Helsinki Foundation.
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