title: Development of molecules stimulating the activity of KLK3 - an update.
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.
authors.forename: Hannu
authors.initials: H
authors.lastname: Koistinen
authors.forename: Erik
authors.initials: E
authors.lastname: Wallén
authors.forename: Henna
authors.initials: H
authors.lastname: Ylikangas
authors.forename: Kristian
authors.initials: K
authors.lastname: Meinander
authors.forename: Maija
authors.initials: M
authors.lastname: Lahtela-Kakkonen
authors.forename: Ale
authors.initials: A
authors.lastname: Närvänen
authors.forename: Ulf-Håkan
authors.initials: UH
authors.lastname: Stenman
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D008297:Male; D008958:Models, Molecular; D010455:Peptides / Q000494:pharmacology; D017430:Prostate-Specific Antigen / Q000737:chemistry / Q000378:metabolism*; D011471:Prostatic Neoplasms / Q000378:metabolism; D059748:Proteolysis / Q000187:drug effects
chemical_list: D010455:Peptides; D017430:Prostate-Specific Antigen