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多元化天然产物用于药物发现的策略。

Strategies to diversify natural products for drug discovery.

机构信息

Department of Natural Medicine and Pharmacognosy, School of Pharmacy, Qingdao University, Qingdao, China.

Department of Natural Products Chemistry, Key Lab of Chemical Biology of Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan, China.

出版信息

Med Res Rev. 2018 Jul;38(4):1255-1294. doi: 10.1002/med.21474. Epub 2017 Oct 24.

Abstract

Natural product libraries contain specialized metabolites derived from plants, animals, and microorganisms that play a pivotal role in drug discovery due to their immense structural diversity and wide variety of biological activities. The strategies to greatly extend natural product scaffolds through available biological and chemical approaches offer unique opportunities to access a new series of natural product analogues, enabling the construction of diverse natural product-like libraries. The affordability of these structurally diverse molecules has been a crucial step in accelerating drug discovery. This review provides an overview of various approaches to exploit the diversity of compounds for natural product-based drug development, drawing upon a series of examples to illustrate each strategy.

摘要

天然产物文库包含源自植物、动物和微生物的特殊代谢物,由于其巨大的结构多样性和广泛的生物活性,在药物发现中起着关键作用。通过现有生物和化学方法极大地扩展天然产物骨架的策略为获得一系列新的天然产物类似物提供了独特的机会,从而构建了多样化的类似天然产物的文库。这些结构多样的分子的可负担性是加速药物发现的关键步骤。本综述概述了利用化合物多样性进行基于天然产物的药物开发的各种方法,通过一系列实例来说明每种策略。

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