中文摘要：

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。

英文摘要：

Prostate cancer is the most prevalent male malignancy in the United States, and remains the second leading cause of cancer-related death in the male population. Prostate specific membrane antigen（PSMA） is a type of II transmembrane glycoproteins that is over-expressed in prostate cancer cell. More importantly, its expression is increased with cancer progression. PSMA has been a major target for imaging and therapeutic applications in prostate cancer. PSMA, also known as N-acetylated α-linked acidic dipeptidase I and folate hydrolase, can catalyze the hydrolysis of α- or γ-linked glutamates from peptides or small molecules. This article provides a review of the recent applications of ligand-drug conjugates targeting PSMA and prodrugs activated by PSMA.