Departments of Chemistry and Molecular & Cell Biology, University of California, Berkeley, 125 Lewis, Berkeley, CA 94720-1460, USA.
Chem Soc Rev. 2014 Sep 21;43(18):6527-36. doi: 10.1039/c4cs00027g.
Both natural products and synthetic organofluorines play important roles in the discovery and design of pharmaceuticals. The combination of these two classes of molecules has the potential to be useful in the ongoing search for new bioactive compounds but our ability to produce site-selectively fluorinated natural products remains limited by challenges in compatibility between their high structural complexity and current methods for fluorination. Living systems provide an alternative route to chemical fluorination and could enable the production of organofluorine natural products through synthetic biology approaches. While the identification of biogenic organofluorines has been limited, the study of the native organisms and enzymes that utilize these compounds can help to guide efforts to engineer the incorporation of this unusual element into complex pharmacologically active natural products. This review covers recent advances in understanding both natural and engineered production of organofluorine natural products.
天然产物和合成有机氟化物在药物的发现和设计中都起着重要的作用。这两类分子的结合有可能在寻找新的生物活性化合物方面发挥作用，但由于其结构复杂性高，与当前氟化方法的兼容性存在挑战，我们生产选择性氟化天然产物的能力仍然有限。生命系统为化学氟化提供了一种替代途径，并可以通过合成生物学方法生产有机氟天然产物。虽然生物源性有机氟的鉴定受到限制，但对利用这些化合物的天然生物体和酶的研究可以帮助指导将这种不寻常元素纳入复杂的具有药理活性的天然产物的工程化。这篇综述涵盖了对天然和工程化生产有机氟天然产物的最新进展的理解。
