用于靶向递送紫杉烷类化合物的改进生化策略。
Improved biochemical strategies for targeted delivery of taxoids.
作者信息
Ganesh Thota
机构信息
Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, GA 30322, USA.
出版信息
Bioorg Med Chem. 2007 Jun 1;15(11):3597-623. doi: 10.1016/j.bmc.2007.03.041. Epub 2007 Mar 18.
Abstract
Paclitaxel (Taxol) and docetaxel (Taxotere) are very important anti-tumor drugs in clinical use for cancer. However, their clinical utility is limited due to systemic toxicity, low solubility and inactivity against drug resistant tumors. To improve chemotherapeutic levels of these drugs, it would be highly desirable to design strategies which bypass the above limitations. In this respect various prodrug and drug targeting strategies have been envisioned either to improve oral bioavailability or tumor specific delivery of taxoids. Abnormal properties of cancer cells with respect to normal cells have guided in designing of these protocols. This review article records the designed biochemical strategies and their biological efficacies as potential taxoid chemotherapeutics.
摘要
紫杉醇（泰素）和多西他赛（泰索帝）是临床上非常重要的抗癌药物。然而，由于全身毒性、低溶解度以及对耐药肿瘤无活性，它们的临床应用受到限制。为了提高这些药物的化疗水平，非常需要设计出能够绕过上述局限性的策略。在这方面，人们设想了各种前药和药物靶向策略，以提高紫杉烷类药物的口服生物利用度或肿瘤特异性递送。癌细胞相对于正常细胞的异常特性为这些方案的设计提供了指导。这篇综述文章记录了作为潜在紫杉烷类化疗药物所设计的生化策略及其生物学疗效。
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