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具有锌结合基团的N-乙酰赖氨酸衍生物作为新型组蛋白去乙酰化酶抑制剂。

N -acetyl lysine derivatives with zinc binding groups as novel HDAC inhibitors.

作者信息

Wang Fang, Wang Chun, Wang Jie, Zou Yefang, Chen Xiaoxue, Liu Ting, Li Yan, Zhao Yonglong, Li Yongjun, He Bin

机构信息

State Key Laboratory of Functions and Applications of Medicinal Plants, Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, People's Republic of China.

School of Pharmacy, Guizhou Medical University, Guiyang 550004, People's Republic of China.

出版信息

R Soc Open Sci. 2019 Jun 5;6(6):190338. doi: 10.1098/rsos.190338. eCollection 2019 Jun.

DOI:10.1098/rsos.190338
PMID:31312496
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6599804/
Abstract

HDAC inhibitors have been developed very rapidly in clinical trials and even in approvals for treating several cancers. However, there are few reported HDAC inhibitors designed from N -acetyl lysine. In the current study, we raised a novel design, which concerns N -acetyl lysine derivatives containing amide acetyl groups with the hybridization of ZBG groups as novel HDAC inhibitors.

摘要

组蛋白去乙酰化酶（HDAC）抑制剂在治疗多种癌症的临床试验甚至获批方面发展迅速。然而，从N - 乙酰赖氨酸设计的HDAC抑制剂报道较少。在本研究中，我们提出了一种新颖的设计，即涉及含有酰胺乙酰基并与锌结合基团（ZBG）杂化的N - 乙酰赖氨酸衍生物作为新型HDAC抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/b2634dc3fdb6/rsos190338-g7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/267e5e5b444a/rsos190338-g1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/1574b8d64bb4/rsos190338-g2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/567f46bc88ae/rsos190338-g3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/78998b86e070/rsos190338-g4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/b3761f5d88fc/rsos190338-g5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/85471cf69bbc/rsos190338-g6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/b2634dc3fdb6/rsos190338-g7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/267e5e5b444a/rsos190338-g1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/1574b8d64bb4/rsos190338-g2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/567f46bc88ae/rsos190338-g3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/78998b86e070/rsos190338-g4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/b3761f5d88fc/rsos190338-g5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/85471cf69bbc/rsos190338-g6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e533/6599804/b2634dc3fdb6/rsos190338-g7.jpg

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