CASIA OpenIR  > 中国科学院分子影像重点实验室
Development of a Novel Ferrocenyl Histone Deacetylase Inhibitor for Triple-Negative Breast Cancer Therapy
Tang Chu; Du Yang; Liang Qian; Cheng Zhen; Tian Jie
Source PublicationOrganometallics
2018
Volume37Issue:14Pages:2368-2375
Abstract

Owing to the lack of target-directed therapies, triple-negative breast cancer (TNBC) is dicult to eectively treat. In this article, a novel organometallic histone deacetylase (HDAC) inhibitor, Fc-SelSA, based on the selenocyanide (SelSA) zinc-binding motif, was synthesized using a ferrocenyl group as the cap to confer activity against TNBC. The synthesized Fc-SelSA was evaluated for bioactivity in vitro and in vivo. An enzymatic assay showed that Fc-SelSA was a potent HDAC inhibitor with a half-maximum inhibitory concentration (IC50) of 14.8 nM. Molecular docking studies of Fc-SelSA with HDAC suggested that the ferrocenyl unit overlaps with the phenyl group of suberoylanilide hydroxamic acid (SAHA) and the amido group of Fc-SelSA can form hydrogen bonds with the D98 and G151 residues of HDAC, but SAHA and SelSA do not show similar interactions. Moreover, Fc-SelSA reactivated the estrogen receptor alpha (ERα) expression, sensitized TNBC cells to the antagonist tamoxifen, and exerted more potent antitumor eects against TNBC MDA-MB-231 tumor xenografts in comparison to SelSA with no obvious side eects. Our results indicate that Fc-SelSA is a potent oral anticancer candidate for HDAC-targeted TNBC therapy and deserves further investigation for clinical application.

KeywordBreast Cancer, Nir Fluorescent Probe, Era-targeted ImagIng, In Vivo Detection
Language英语
Document Type期刊论文
Identifierhttp://ir.ia.ac.cn/handle/173211/23179
Collection中国科学院分子影像重点实验室
Corresponding AuthorCheng Zhen; Tian Jie
Recommended Citation
GB/T 7714
Tang Chu,Du Yang,Liang Qian,et al. Development of a Novel Ferrocenyl Histone Deacetylase Inhibitor for Triple-Negative Breast Cancer Therapy[J]. Organometallics,2018,37(14):2368-2375.
APA Tang Chu,Du Yang,Liang Qian,Cheng Zhen,&Tian Jie.(2018).Development of a Novel Ferrocenyl Histone Deacetylase Inhibitor for Triple-Negative Breast Cancer Therapy.Organometallics,37(14),2368-2375.
MLA Tang Chu,et al."Development of a Novel Ferrocenyl Histone Deacetylase Inhibitor for Triple-Negative Breast Cancer Therapy".Organometallics 37.14(2018):2368-2375.
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