A 5-fluorodeoxyuridine prodrug as targeted therapy for prostate cancer
A 5-fluorodeoxyuridine prodrug as targeted therapy for prostate cancer
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DOI：
10.1016/s0960-894x(02)00433-x
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发表时间：
2002-09-02
影响因子：
2.7
通讯作者：
Khan, SR
中科院分区：
文献类型：
--
作者：
Mhaka, A;Denmeade, SR;Khan, SR
描述了一种将细胞毒性剂5-氟脱氧尿苷（FudR）（1）靶向递送至转移性前列腺癌部位的方法。通过将活性药物（FudR）经由自裂解二氨基酸接头偶联至PSA-肽以产生HSSKLQ-Leu-Aib-FudR来合成前药。该前药作为前列腺特异性抗原（PSA）的底物。这种方法允许通过前列腺细胞高度表达的PSA的酶活性将无活性前药有效转化回活性细胞毒性状态。(C)2002爱思唯尔科技有限公司版权所有。
A method for targeted delivery of the cytotoxic agent 5-fluorodeoxyuridine (FudR) (1) to sites of metastatic prostate cancer is described. The prodrug was synthesized by coupling the active drug (FudR) to the PSA-peptide via a self-cleaving diamino acid linker to produce HSSKLQ-Leu-Aib-FudR. This prodrug serves as a substrate for prostate specific antigen (PSA). This approach permitted efficient conversion of the inactive prodrug back to the active cytotoxic state by the enzymatic activity of PSA which is highly expressed by prostate cells. (C) 2002 Elsevier Science Ltd. All rights reserved.