[关键词]
[摘要]
成纤维细胞活化蛋白(FAP)是肿瘤相关成纤维细胞表面重要的标志物之一,在90%以上的上皮癌的基质成纤维细胞中高表达,在肿瘤的发生和发展中发挥着重要的作用。FAP属于DPPⅣ蛋白家族,能特异性水解Gly-Pro序列后的脯氨酸和其他小分子形成的肽键。FAP作为肿瘤治疗的靶点已经在多方面进行研究,主要介绍基于FAP靶点的酶激活式抗肿瘤前体药物的研究进展。
[Key word]
[Abstract]
FAP (fibroblast activation protein), one of the most important markers of cancer associated fibroblasts, overexpresses in more than 90% stromal fibroblasts of epithelial carcinoma. It plays an important role in the genesis and development of cancer. FAP belongs to the DPP Ⅳ family. A remarkable exhibition of dipeptidase activity of FAP is its ability to cleave various molecules from polypeptide after proline in the Gly-Pro sequence. Therapeutic approaches targeting to FAP have been researched from different aspects. Research progress on enzyme activated antitumor prodrugs based on FAP are reviewed in this article.
[中图分类号]
[基金项目]
国家自然科学基金资助项目(31470423);广东省公益研究与能力建设资助项目(2017A020208031);广东省农业科学院院长基金资助项目(201616)