成纤维细胞活化蛋白（FAP）是一种II型跨膜丝氨酸蛋白酶，参与了肿瘤的发生、发展和迁移。小分子FAP抑制剂在肿瘤的进展和预后中发挥重要作用，成为检测和治疗恶性肿瘤的有效策略。对小分子硼酸类、喹啉类、环肽类和多聚体FAP抑制剂在肿瘤靶向诊疗中的应用，以及在亲和力、选择性、构效关系、体内代谢和临床研究进行综述，以期为肿瘤的精准治疗提供新的视角和策略。

Fibroblast activating protein (FAP) is a type II transmembrane serine protease that is involved in the occurrence, development, and migration of tumors. Small molecule FAP inhibitors play an important role in the progression and prognosis of tumors, becoming an effective strategy for detecting and treating malignant tumors. This article reviews the application of small molecule boronic acid, quinolines, cyclic peptides, and polymeric FAP inhibitors in targeted diagnosis and treatment of tumors, as well as their affinity, selectivity, conformational relationship, in vivo metabolism, and clinical research, in order to provide new perspectives and strategies for precision treatment of tumors.

R966

国家自然科学基金资助项目（82104012）