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The human tissue kallikrein gene family contains 15 members that play important roles in cancer. Notably, KLK1, also known as tissue kallikrein, cleaves kininogen to release the vasoactive kinin peptide, bradykinin or lysyl-bradykinin. KLK3, called prostate specific antigen (PSA), is an established tumor marker that aids in the diagnosis, staging, and follow up of prostate cancer. KLK4 is specifically expressed in the prostate and overexpressed in prostate cancer. KLK5 is widely expressed but found at high levels in skin, breast, brain and testis; overexpression is an indicator of poor prognosis in ovarian cancer. KLK8 is expressed in the brain and is a novel marker of ovarian and cervical cancer.