Clinical Research Unit, Department of Obstetrics and Gynecology, Klinikum rechts der Isar, Technische Universität München, Munich, Germany.
Radiol Oncol. 2013 Oct 8;47(4):319-29. doi: 10.2478/raon-2013-0053. eCollection 2013.
Tumor tissue-associated KLKs (kallikrein-related peptidases) are clinically important biomarkers that may allow prognosis of the cancer disease and/or prediction of response/failure of cancer patients to cancer-directed drugs. Regarding the female/male reproductive tract, remarkably, all of the fifteen KLKs are expressed in the normal prostate, breast, cervix uteri, and the testis, whereas the uterus/endometrium and the ovary are expressing a limited number of KLKs only.
Most of the information regarding elevated expression of KLKs in tumor-affected organs is available for ovarian cancer; depicting them as valuable biomarkers in the cancerous phenotype. In contrast, for breast cancer, a series of KLKs was found to be downregulated. However, in breast cancer, KLK4 is elevated which is also true for ovarian and prostate cancer. In such cases, selective synthetic KLK inhibitors that aim at blocking the proteolytic activities of certain KLKs may serve as future candidate therapeutic drugs to interfere with tumor progression and metastasis.
肿瘤组织相关激肽释放酶（KLKs， Kallikrein-related peptidases）是临床重要的生物标志物，可能有助于预测癌症疾病的预后，以及预测癌症患者对癌症靶向药物的反应/失败。关于女性/男性生殖道，值得注意的是，十五种 KLKs 均在正常前列腺、乳腺、子宫颈和睾丸中表达，而子宫/子宫内膜和卵巢仅表达有限数量的 KLKs。
大多数关于卵巢癌中 KLKs 表达升高的信息可作为有价值的生物标志物用于癌症表型。相比之下，在乳腺癌中，发现一系列 KLKs 下调。然而，在乳腺癌中，KLK4 升高，在卵巢癌和前列腺癌中也是如此。在这种情况下，选择性合成 KLK 抑制剂，旨在阻断某些 KLKs 的蛋白水解活性，可能成为未来候选治疗药物，以干扰肿瘤的进展和转移。
