Paclitaxel rapidly became one of the most effective anticancer drugs. However, the production of paclitaxel is hindered by substantial challenges, particularly considering the significant quantities of drug required and the inherently low concentration of paclitaxel and its intermediates in plants. Paclitaxel is currently produced in a so-called semi-synthesis in which baccatin III is extracted from Taxus species and chemically converted to paclitaxel. Despite the fact that many of the intermediates of paclitaxel biosynthesis are yet to be experimentally determined, a set of recent papers—facilitated by the sequencing and assembly of three Taxus genomes—has uncovered the minimal gene sets for both baccatin III and paclitaxel biosynthesis. Here we summarize the key milestones towards our understanding of paclitaxel biosynthesis and highlight recent advancements made possible by genome-level analysis of potential key genes involved. We argue that these studies will ultimately pave the way towards the elucidation of the entire paclitaxel biosynthetic pathway and facilitate the industrial production of paclitaxel via synthetic biology approaches. However, several major challenges lie ahead before we can fully tap into the amazing curative potential that taxanes provide.

紫杉醇迅速成为最有效的抗癌药物之一。然而，紫杉醇的生产受到重大挑战的阻碍，特别是考虑到所需的大量药物以及紫杉醇及其中间体在植物中的固有低浓度。紫杉醇目前以所谓的半合成方式生产，其中巴卡汀 III 从红豆杉属中提取并化学转化为紫杉醇。尽管紫杉醇生物合成的许多中间体尚未通过实验确定，但最近的一组论文——通过三个红豆杉基因组的测序和组装——揭示了巴卡汀 III 和紫杉醇生物合成的最小基因集。在这里，我们总结了我们理解紫杉醇生物合成的关键里程碑，并强调了通过对所涉及的潜在关键基因进行基因组水平分析而取得的最新进展。我们认为，这些研究最终将为阐明整个紫杉醇生物合成途径铺平道路，并通过合成生物学方法促进紫杉醇的工业化生产。然而，在我们能够充分利用紫杉烷类药物提供的惊人治疗潜力之前，还有几个主要挑战摆在我们面前。