蓝基因学：具有医学相关性的生物活性天然产物及其多样化方法。

Bluegenics: Bioactive Natural Products of Medicinal Relevance and Approaches to Their Diversification.

作者信息

Zarins-Tutt Joseph S, Abraham Emily R, Bailey Christopher S, Goss Rebecca J M

机构信息

School of Chemistry, University of St Andrews, St Andrews, Scotland, UK.

出版信息

Prog Mol Subcell Biol. 2017;55:159-186. doi: 10.1007/978-3-319-51284-6_5.

DOI:10.1007/978-3-319-51284-6_5

PMID:28238038

Abstract

Nature provides a valuable resource of medicinally relevant compounds, with many antimicrobial and antitumor agents entering clinical trials being derived from natural products. The generation of analogues of these bioactive natural products is important in order to gain a greater understanding of structure activity relationships; probing the mechanism of action, as well as to optimise the natural product's bioactivity and bioavailability. This chapter critically examines different approaches to generating natural products and their analogues, exploring the way in which synthetic and biosynthetic approaches may be blended together to enable expeditious access to new designer natural products.

摘要

大自然提供了宝贵的与医学相关的化合物资源，许多进入临床试验的抗菌和抗肿瘤药物都源自天然产物。生成这些生物活性天然产物的类似物对于更深入了解构效关系、探究作用机制以及优化天然产物的生物活性和生物利用度非常重要。本章批判性地审视了生成天然产物及其类似物的不同方法，探讨了如何将合成方法和生物合成方法结合起来，以便快速获得新型设计天然产物。