成纖維細(xì)胞活化蛋白（FAP）是一種II型跨膜絲氨酸蛋白酶，參與了腫瘤的發(fā)生、發(fā)展和遷移。小分子FAP抑制劑在腫瘤的進(jìn)展和預(yù)后中發(fā)揮重要作用，成為檢測(cè)和治療惡性腫瘤的有效策略。對(duì)小分子硼酸類、喹啉類、環(huán)肽類和多聚體FAP抑制劑在腫瘤靶向診療中的應(yīng)用，以及在親和力、選擇性、構(gòu)效關(guān)系、體內(nèi)代謝和臨床研究進(jìn)行綜述，以期為腫瘤的精準(zhǔn)治療提供新的視角和策略。

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

國(guó)家自然科學(xué)基金資助項(xiàng)目（82104012）