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, Chu1,2; Du, Yang2,3,4; Liang, Qian2; Cheng, Zhen5,6; Tian, Jie1,2,3,4
Source PublicationORGANOMETALLICS
2018-07-23
Volume37Issue:14Pages:2368-2375
SubtypeArticle
AbstractOwing to the lack of target-directed therapies, triple-negative breast cancer (TNBC) is difficult to effectively 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-SeISA was evaluated for bioactivity in vitro and in vivo. An enzymatic assay showed that Fc-SeISA 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 (ER alpha) expression, sensitized TNBC cells to the antagonist tamoxifen, and exerted more potent antitumor effects against TNBC MDA-MB-231 tumor xenografts in comparison to SelSA with no obvious side effects. Our results indicate that Fc-SeISA is a potent oral anticancer candidate for HDAC-targeted TNBC therapy and deserves further investigation for clinical application.
WOS HeadingsScience & Technology ; Physical Sciences
DOI10.1021/acs.organomet.8b00354
WOS Keyword1ST GLOBAL APPROVAL ; ESTROGEN-RECEPTOR ; ANTIPROLIFERATIVE ACTIVITY ; HDAC INHIBITORS ; CELL-LINES ; METABOLISM ; DISEASE ; HYBRIDS
Indexed BySCI
Language英语
Funding OrganizationMinistry of Science and Technology of China(2017YFA0205200 ; National Natural Science Foundation of China(81470083 ; International Innovation Team of CAS(20140491524) ; Beijing Municipal Science & Technology Commission(Z161100002616022) ; Fundamental Research Funds for the Central universities(JB161204 ; China Postdoctoral Science Foundation(2017M613084) ; Shaanxi Postdoctoral Science Foundation(2017BSHEDZZ91) ; 2016YFC0102000) ; 81527805 ; JBG161201 ; 61231004 ; XJS16011) ; 81601548 ; 81701771 ; 81772011)
WOS Research AreaChemistry
WOS SubjectChemistry, Inorganic & Nuclear ; Chemistry, Organic
WOS IDWOS:000439955400019
Citation statistics
Document Type期刊论文
Identifierhttp://ir.ia.ac.cn/handle/173211/21843
Collection中国科学院分子影像重点实验室
Affiliation1.Xidian Univ, Engn Res Ctr Mol & Neuro Imaging, Sch Life Sci & Technol, Minist Educ, Xian 710126, Shaanxi, Peoples R China
2.Chinese Acad Sci, Inst Automat, State Key Lab Management & Control Complex Syst, CAS Key Lab Mol Imaging, Beijing 100190, Peoples R China
3.Beijing Key Lab Mol Imaging, Beijing 100190, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100080, Peoples R China
5.Stanford Univ, Canary Ctr Stanford Canc Early Detect, Dept Radiol, MIPS, Stanford, CA 94305 USA
6.Stanford Univ, Canary Ctr Stanford Canc Early Detect, Bio X Program, Stanford, CA 94305 USA
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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