Xie Shaowen, Zhan Fangyi, Zhu Jingjie, Xu Shengtao, Xu Jinyi
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, China.
Expert Opin Drug Discov. 2025 Jul;20(7):827-843. doi: 10.1080/17460441.2025.2507382. Epub 2025 Jun 5.
The landscape of drug discovery is rapidly evolving, with natural products (NPs) playing a pivotal role in the development of novel therapeutics. Despite their historical significance, challenges persist in fully harnessing their potential in the development of modern medicine.
This perspective discusses the recent advances and opportunities in NP-based drug discovery. This includes exploration of the recently approved representative NP-derived drugs, innovative target identification strategies and advancements in hybrid NP molecules for addressing complex diseases. Moreover, the authors also discuss the role of NP-derived payloads in antibody-drug conjugates (ADCs) for targeted cancer therapy. This article is based on searches using the FDA and DrugBank database as well the Derwent Innovations Index from Web of Science between the period of 2017 to 2025.
NPs remain vital to drug discovery, demonstrating adaptability in tackling complex medical challenges. Future efforts should focus on integrating advanced methodologies, such as artificial intelligence (AI), high-throughput screening, chemical biology, bioinformatics, gene regulation, the highly accurate non-labeling chemical proteomics approach to explore novel NPs targets. Emphasizing these developments will be crucial for maximizing the therapeutic potential of NPs in combating unmet medical needs.
药物研发领域正在迅速发展，天然产物（NPs）在新型治疗药物的开发中发挥着关键作用。尽管它们具有历史意义，但在现代医学开发中充分发挥其潜力仍存在挑战。
本观点讨论了基于天然产物的药物研发的最新进展和机遇。这包括对最近获批的具有代表性的天然产物衍生药物的探索、创新的靶点识别策略以及用于治疗复杂疾病的杂合天然产物分子的进展。此外，作者还讨论了天然产物衍生的有效载荷在用于靶向癌症治疗的抗体药物偶联物（ADC）中的作用。本文基于使用美国食品药品监督管理局（FDA）和药物银行（DrugBank）数据库以及2017年至2025年期间科学网（Web of Science）的德温特创新索引（Derwent Innovations Index）进行的检索。
天然产物对于药物研发仍然至关重要，在应对复杂医学挑战方面展现出适应性。未来的努力应集中于整合先进方法，如人工智能（AI）、高通量筛选、化学生物学、生物信息学、基因调控、高度精确的非标记化学蛋白质组学方法，以探索新型天然产物靶点。强调这些进展对于最大化天然产物在满足未满足医疗需求方面的治疗潜力至关重要。
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