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金属基质蛋白酶(MMP)作为锌依赖性肽链内切酶,家族成员繁多,与肿瘤的发生发展密切相关,所以经常将MMP作为抗癌靶点进行药物研究。早期的MMP靶点类抗癌药物是MMP的天然抑制蛋白——MMP组织抑制剂(TIMP),后来通过研究又发现了很多化学分子抑制剂(如马马司他、坦诺司他、普啉司他),但这些化学药物临床有效性和安全性较差,很难应用于临床。多肽类抑制剂由于具有相对分子质量小、结合效率高等优点比较适合作为金属基质蛋白酶的分子抑制剂或靶向释药载体。本文对MMP这一靶点和抗癌药物的研究进展进行介绍。
As a zinc-dependent endopeptidase, the matrix metalloproteinases (MMPs) have many families and are closely related to tumorigenesis and development. Therefore, MMPs are often used as anticancer targets for drug research. Early anti-cancer MMP target drugs are MMPs natural inhibitor protein - MMP tissue inhibitor (TIMP), and later found through the study and a lot of chemical inhibitors (such as mastatine, tannastat, Sto), but the clinical efficacy and safety of these chemicals is poor, it is difficult to apply to clinical. Polypeptide inhibitors are more suitable as molecular inhibitors of metal matrix protease or targeted drug release carriers due to their advantages of small relative molecular mass and high binding efficiency. This article describes the progress of MMP research and anticancer drugs.