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。

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.

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）