Prodrugs for improving tumor targetability and efficiency.
Prodrugs for improving tumor targetability and efficiency.
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DOI：
10.1016/j.addr.2011.02.002
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发表时间：
2011-07-18
影响因子：
16.1
通讯作者：
Cheng, Kun
中科院分区：
文献类型：
--
作者：
Mahato, Rubi;Tai, Wanyi;Cheng, Kun
作为几十年来治疗各种癌症的主要手段，化疗是成功的，但仍然面临着包括非选择性和高毒性在内的挑战。因此，提高选择性是提高化疗疗效的关键步骤。前药是提高化疗药物选择性和疗效的最有前途的方法之一。经典的前药方法是改善药物性质（溶解性、稳定性、渗透性、刺激性、分布等）。通过简单的化学修饰这篇综述将集中在各种有针对性的前药设计，已开发的化疗药物的选择性增加。各种肿瘤靶向配体、转运蛋白相关配体和聚合物可掺入前药中以增强肿瘤摄取。前药也可以被在肿瘤中以更高水平特异性表达的酶激活，导致选择性抗肿瘤作用。这可以通过将酶与肿瘤特异性抗体缀合或将表达酶的载体递送到肿瘤细胞中来实现。
As the mainstay in the treatment of various cancers for several decades, chemotherapy is successful but still faces challenges including non-selectivity and high toxicity. Improving the selectivity is therefore a critical step to improve the therapeutic efficacy of chemotherapy. Prodrug is one of the most promising approaches to increase the selectivity and efficacy of a chemotherapy drug. The classical prodrug approach is to improve the pharmaceutical properties (solubility, stability, permeability, irritation, distribution, etc.) via a simple chemical modification. This review will focus on various targeted prodrug designs that have been developed to increase the selectivity of chemotherapy drugs. Various tumor-targeting ligands, transporter-associated ligands, and polymers can be incorporated in a prodrug to enhance the tumor uptake. Prodrugs can also be activated by enzymes that are specifically expressed at a higher level in tumors, leading to a selective anti-tumor effect. This can be achieved by conjugating the enzyme to a tumor-specific antibody, or delivering a vector expressing the enzyme into tumor cells.
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DOI：
10.1124/jpet.105.100347
发表时间：
2006-05-01
影响因子：
3.5
作者：
Cheng, K;Ye, ZY;Mahato, RI
通讯作者：
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影响因子：
11.5
作者：
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影响因子：
45.3
作者：
Chévez-Barrios, P;Chintagumpala, M;Hurwitz, RL
通讯作者：
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DOI：
10.1073/pnas.0504274102
发表时间：
2005-09-06
影响因子：
11.1
作者：
Dharap, SS;Wang, Y;Minko, T
通讯作者：
Minko, T
适体介导的siRNA传递。
影响因子：
14.9
作者：
Chu, Ted C.;Twu, Karen Y.;Ellington, Andrew D.;Levy, Matthew
通讯作者：
Levy, Matthew