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Chemical and Biological Integrity in Natural Products Screening

机译：天然产物筛选中的化学和生物完整性

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摘要

Due to pressure from combinatorial chemistry and the streamlining of the drug discovery processnthrough automated high-throughput screening technologies, pharmaceutically based natural productsnprograms are under increasing scrutiny. However by taking advantages of technologies originally developednfor high-throughput screening and combinatorial chemistry and applying them to processes considered asnbottlenecks in classical natural products chemistry (purification, structure elucidation, sample availability) itnis our opinion that natural products can still contribute to the effective discovery of novel bioactive andnpharmaceutically relevant metabolites. We describe here several such strategies that if universallynimplemented, will demonstrate i) whether chemical diversity is truly being accessed, ii) that novel metabolitesncan be formatted in a manner appropriate for modern screening paradigms, and iii) that natural products can benrapidly identified not only for novelty and pharmaceutical relevance but to assess their true biological origin.
机译：由于来自组合化学的压力以及通过自动化高通量筛选技术简化药物开发过程的结果，基于药物的天然产物程序正在受到越来越多的审查。但是，通过利用最初为高通量筛选和组合化学开发的技术的优势，并将其应用于经典天然产物化学中被视为瓶颈的过程（纯化，结构解析，样品可得性），我们认为天然产物仍然可以有效地发现新的生物活性和药学相关的代谢产物。我们在这里描述了几种这样的策略，这些策略如果得到普遍实施，将证明i）是否真正利用了化学多样性，ii）可以以适合现代筛选范式的方式格式化新的代谢产物，并且iii）不仅可以针对新颖性和药物相关性，但要评估其真正的生物学起源。

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