Hans Lilja, MD, PhD, Memorial Sloan-Kettering Cancer Center, 1275 York Ave Box 213, New York, NY 10065, USA, Tel.: +1 212 639 6982, Fax: +1 646 422 2379, E-mail:
Thromb Haemost. 2013 Sep;110(3):484-92. doi: 10.1160/TH13-04-0275. Epub 2013 Aug 1.
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.
激肽释放酶是一族丝氨酸蛋白酶，具有多种组织特异性和重要的蛋白水解功能。其中研究得最多的是前列腺组织特异性 KLK2 和 KLK3 基因及其分泌的蛋白酶产物，人激肽释放酶 2（hk2）和前列腺特异性抗原（PSA）。这些所谓的经典激肽释放酶成员是高度活跃的胰蛋白酶样丝氨酸蛋白酶，在人类生殖中发挥着既定的作用。hK2 和 PSA 的表达均受雄激素受体调控，雄激素受体在前列腺组织发育和疾病进展中起着至关重要的作用。这一特征，加上能够在血液和活检中灵敏地检测到这些蛋白质的不同形式，使它们成为癌症存在和复发的重要生物标志物。新出现的证据开始表明这些激肽释放酶在关键的血管事件中发挥作用。本文讨论了 hK2 和 PSA 的既定和不断发展的生物学作用，以及它们的检测在准确和非侵入性地检测和指导前列腺疾病治疗方面的历史和先进应用。
