Drug targeting via retrometabolic approaches
Drug targeting via retrometabolic approaches
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DOI：
10.1016/s0163-7258(97)00098-3
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发表时间：
1997-10-01
影响因子：
13.5
通讯作者：
Buchwald, P
中科院分区：
文献类型：
--
作者：
Bodor, N;Buchwald, P
逆代谢方法将靶向和代谢考虑因素纳入药物设计过程中，代表了一种用于设计安全、局部化合物的新颖、系统的方法。开发了两个旨在提高药物治疗指数的主要设计概念。化学递送系统允许基于可预测的酶促激活将活性生物分子靶向特定的靶位点或器官。软药物方法用于通过构建分子来设计新药，除了活性之外，最理想的方式是分子在发挥其生物效应后失活和解毒。提供了很多例子；还简要讨论了相关的计算机程序。 (C) 1997 爱思唯尔科学公司。
Retrometabolic approaches incorporate targeting and metabolic considerations into the drug design process and represent a novel, systematic methodology for the design of safe, localized compounds. Two major design concepts aimed to increase the therapeutic index of drugs were developed. Chemical delivery systems allow targeting of active biological molecules to specific target sites or organs, based on predictable enzymatic activation. Soft drug approaches are used to design new drugs by building in the molecule, in addition to the activity, the most desired way in which the molecule is to be deactivated and detoxified subsequent to exerting its biological effects. Many examples are provided; related computer programs are also briefly discussed. (C) 1997 Elsevier Science Inc.