摘要
新型抗疟药物研发中,组蛋白去乙酰化酶被证明是有效的抗疟新靶点。本文介绍了组蛋白去乙酰化酶抑制剂的作用机制及其抗疟活性,重点概述了疟原虫组蛋白去乙酰化酶抑制剂发现过程和国内外研究进展,按照不同的结构类型,对异羟肟酸类、环肽类抑制剂近些年的研究成果进行了详细介绍和分析,提出了药物毒性问题、相关生物学研究滞后等制约药物开发上市的关键因素,并对药物未来的研发方向进行展望,为进一步开发抗疟新药提供思路。
Histone deacetylase has proved to be a promising new antimalarial target in the development of novel antimalarial drugs.This article introduces the mechanism of action of histone deacetylase inhibitors and their antimalarial activity,with a focus on the discovery process of Plasmodium histone deacetylase inhibitors and their recent research progress both domestically and internationally.Recent research findings on hydroxamic acidbased and cyclic peptide inhibitors are reviewed and analyzed in detail according to their different structural types.Key challenges hindering drug development and approval,such as drug toxicity issues and the lag in related biological studies,are highlighted.Furthermore,future directions for drug research and development are proposed,offering insights for the further development of new antimalarial drugs.
作者
赵磊
张梦蝶
孙鹏
ZHAO Lei;ZHANG Mengdie;SUN Peng(Center for Drug Evaluation,National Medical Products Administration,Beijing 102600;Artemisinin Research Center,China Academy of Chinese Medical Science,Beijing 100700,China)
出处
《中国药科大学学报》
北大核心
2026年第1期28-33,共6页
Journal of China Pharmaceutical University
基金
中央公益性科研院所基本科研业务费项目(ZZ13-YQ-098)。
