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前列腺癌是男性最常见的恶性肿瘤之一,在美国前列腺癌的发病率在男性肿瘤中排名第一,死亡率排名第二。前列腺特异性膜抗原是存在于前列腺上皮细胞膜的一种II型跨膜糖蛋白,它在前列腺癌中高度表达,尤其是转移前列腺癌及激素抵抗前列腺癌,在前列腺癌的诊断和靶向治疗中显示出良好的应用前景。此外,前列腺特异性膜抗原还具有叶酸水解酶和N-乙酰基-α-连接二肽酶I活性,能够催化α或γ键连接的谷氨酸从肽或小分子物质上水解出来。本文重点对以前列腺特异性膜抗原为靶标的配体-药物偶联物和前列腺特异性膜抗原激活前药的最新研究进展进行综述。
Prostate cancer is one of the most common malignant tumors in men. In the United States, the incidence of prostate cancer ranks the first among men’s tumors with the second highest mortality rate. Prostate-specific membrane antigen is a Type II transmembrane glycoprotein present in the prostate epithelial cell membrane and is highly expressed in prostate cancer, especially in metastatic prostate cancer and hormone-refractory prostate cancer. In the diagnosis and targeted therapy of prostate cancer Shows a good application prospects. In addition, prostate-specific membrane antigens also have folate hydrolase and N-acetyl-α-linked dipeptidase I activities that catalyze the hydrolysis of α or γ-linked glutamate from peptides or small molecules. This review focuses on recent advances in ligand-drug conjugates that target prostate-specific membrane antigens and prostate-specific membrane antigen-activated prodrugs.