summary
Kallikreins are a family of serine proteases with a range of tissue-specific and essential
proteolytic functions. Among the best studied are the prostate tissue-specific KLK2 and KLK3 genes and their secreted protease products, human kallikrein 2, hk2, and prostate-specific
antigen (PSA). Members of the so-called classic kallikreins, these highly active trypsin-like
serine proteases play established roles in human reproduction. Both hK2 and PSA expression
is regulated by the androgen receptor which has a fundamental role in prostate tissue
development and progression of disease. This feature, combined with the ability to
sensitively detect different forms of these proteins in blood and biopsies, result
in a crucially important biomarker for the presence and recurrence of cancer. Emerging
evidence has begun to suggest a role for these kallikreins in critical vascular events.
This review discusses the established and developing biological roles of hK2 and PSA,
as well as the historical and advanced use of their detection to accurately and non-invasively
detect and guide treatment of prostatic disease.