Recent progress in chemistry and bioactivity of novel enzyme inhibitors from natural products: A comprehensive review

IF 5.9 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2025-03-07 DOI:10.1016/j.ejmech.2025.117481
Chengqian Pan , Hideaki Kakeya
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Abstract

The essence of enzymes is to maintain the normal activities of living organisms by catalyzing metabolic reactions and regulating cells. Inhibiting enzyme activity can slow the progression of certain diseases and cure them, making enzymes one of the major targets for disease treatment. The search and development of novel enzyme inhibitors are of great significance for the treatment of certain major diseases. One of the most prominent features of natural products is their complex and diverse structures, which often compliments the synthetic capabilities of medicinal chemistry. Considering the biosynthetic processes of natural molecules in organisms, they exhibit higher similarity and binding potential with biological structures, enabling them to serve as ligands for various enzymes and receptors. In this review, we summarized a total of 226 novel natural products with enzyme inhibitory activity published in 49 articles over the past three years (2022–2024). These natural products (including terpenes, alkaloids, flavonoids, phenylpropanoids, polyketides, peptides, anthraquinones, etc.) are derived from plants, microorganisms, and marine organisms. We also discuss some synthetic analogs, with a focus on their structures and biological activities. This review provides useful information for the research and development of novel enzyme inhibitors.

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天然产物中新型酶抑制剂的化学和生物活性研究进展综述
酶的本质是通过催化代谢反应和调节细胞来维持生物体的正常活动。抑制酶活性可以减缓某些疾病的进展并治愈它们,使酶成为疾病治疗的主要靶点之一。寻找和开发新型酶抑制剂对某些重大疾病的治疗具有重要意义。天然产物最突出的特征之一是其复杂多样的结构,这往往与药物化学的合成能力相辅相成。考虑到生物体内天然分子的生物合成过程,它们与生物结构具有较高的相似性和结合潜力,使其能够作为各种酶和受体的配体。在这篇综述中,我们总结了过去三年(2022-2024)49篇文章中发表的226种具有酶抑制活性的新型天然产物。这些天然产物(包括萜烯、生物碱、类黄酮、苯丙素、聚酮、肽、蒽醌等)来源于植物、微生物和海洋生物。我们还讨论了一些合成类似物,重点讨论了它们的结构和生物活性。本文综述为新型酶抑制剂的研究和开发提供了有益的信息。
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来源期刊
CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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