Nelles L P, Schnebli H P
Invasion Metastasis. 1982;2(2):113-24.
Within the last 15 years a vast literature has arisen, which associates increased levels of proteinase activity with most in vitro transformed malignant cells and many tumor cells in vivo. As a consequence, proteinase inhibitors have been widely proposed as potential candidates for therapeutic use. The present review shows that in some studies proteinase inhibitors produced significant anti-tumor effects, while in most other studies only limited effects or no effects were observed. In some instances, opposite, or tumor enhancing, effects by proteinase inhibitors were observed. The reasons for the lack of a clear-cut success of proteinase inhibitors in tumor therapy may be: (1) proteinases may not be crucially involved in tumor growth and spread; (2) proteinases which may be crucially involved have not yet been identified; (3) lack of potent inhibitors with appropriate specificity, or use of inappropriate inhibitors or regimens.
在过去15年里，涌现出了大量文献，这些文献将蛋白酶活性水平的升高与大多数体外转化的恶性细胞以及体内许多肿瘤细胞联系起来。因此，蛋白酶抑制剂已被广泛提议作为潜在的治疗用药。本综述表明，在一些研究中蛋白酶抑制剂产生了显著的抗肿瘤作用，而在大多数其他研究中仅观察到有限的作用或无作用。在某些情况下，还观察到蛋白酶抑制剂产生了相反的或促进肿瘤的作用。蛋白酶抑制剂在肿瘤治疗中缺乏明确成功的原因可能是：（1）蛋白酶可能并非肿瘤生长和扩散的关键因素；（2）可能是关键因素的蛋白酶尚未被识别；（3）缺乏具有适当特异性的有效抑制剂，或使用了不合适的抑制剂或治疗方案。
