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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Designing multi-targeted agents: An emerging anticancer drug discovery paradigm
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Designing multi-targeted agents: An emerging anticancer drug discovery paradigm

机译：设计多目标代理商：新兴抗癌药物发现范式

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摘要

The dominant paradigm in drug discovery is to design ligands with maximum selectivity to act on individual drug targets. With the target-based approach, many new chemical entities have been discovered, developed, and further approved as drugs. However, there are a large number of complex diseases such as cancer that cannot be effectively treated or cured only with one medicine to modulate the biological function of a single target. As simultaneous intervention of two (or multiple) cancer progression relevant targets has shown improved therapeutic efficacy, the innovation of multi-targeted drugs has become a promising and prevailing research topic and numerous multi-targeted anticancer agents are currently at various developmental stages. However, most multi-pharmacophore scaffolds are usually discovered by serendipity or screening, while rational design by combining existing pharmacophore scaffolds remains an enormous challenge. In this review, four types of multi-pharmacophore modes are discussed, and the examples from literature will be used to introduce attractive lead compounds with the capability of simultaneously interfering with different enzyme or signaling pathway of cancer progression, which will reveal the trends and insights to help the design of the next generation multi-targeted anticancer agents. (C) 2017 Elsevier Masson SAS. All rights reserved.
机译：药物发现中的主导范式是设计具有最大选择性的配体，以对个体药物目标采取行动。利用基于目标的方法，已经发现了许多新化学实体，开发，进一步批准为药物。然而，存在大量复杂的疾病，例如癌症，这些疾病是不能有效处理或固化的癌症，只用一种药物调节单个靶的生物学功能。随着两种（或多个）癌症进展的同时干预相关目标表现出改善的治疗疗效，多目标药物的创新已成为一个有前途和普遍的研究课题，许多多目标抗癌剂目前处于各种发展阶段。然而，大多数多药镜支架通常通过偶然或筛选来发现，而通过组合现有的药物支架结构的理性设计仍然是一个巨大的挑战。在该评价中，讨论了四种类型的多药疗法模式，文献中的实施例将用于引入有吸引力的铅化合物，其能够同时干扰癌症进展的不同酶或信号通路，这将揭示趋势和见解帮助设计下一代多目标抗癌代理商。 （c）2017年Elsevier Masson SAS。版权所有。

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