Pyrrolo [3,4-b]-quinolin-9-amine compound FZU-0038-056 suppresses triple-negative breast cancer partially through inhibiting the expression of Bcl-2 - Details

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Abstract：

Triple-negative　breast　cancer　(TNBC)　has　a　poorer　prognosis　than　other　subtypes　of　breast　cancer;　however,　it　lacks　effective　targeted　therapies　clinically.　In　this　study,　we　found　FZU-0038-056,　a　novel　compound　derived　from　last-stage　functionalization　of　tetrahydro-β-carboline　scaffold,　showed　the　most　potent　anti-cancer　activity　against　TNBC　cells　among　the　42　synthesized　derivatives.　We　found　FZU-0038-056　significantly　induces　apoptosis　in　HCC1806　and　HCC1937　TNBC　cells.　FZU-0038-056　reduces　the　expression　levels　of　several　anti-apoptosis　proteins,　including　Bcl-2,　Mcl-1　and　XIAP.　Furthermore,　we　found　FZU-0038-056　induces　apoptosis　partially　through　inhibiting　the　expression　of　Bcl-2.　Finally,　we　found　FZU-0038-056　significantly　suppresses　HCC1806　xenograft　tumor　growth　in　nude　mice　without　affecting　their　body　weight.　Therefore,　FZU-0038-056　has　the　potential　to　be　a　new　anticancer　agent　for　treating　human　TNBC.　©　2020,　Wang　et　al.

Keyword：

Apoptosis; Bcl-2; Tetrahydro-ß-carboline derivatives; Triple-negative breast cancer

Community：

[ 1 ] [Wang, D.]Department of Pathology, First Affiliated Hospital of Kunming Medical University, Kunming, Yunnan, 650032, China
[ 2 ] [Nie, Z.]Department of Neurology, First Affiliated Hospital of Kunming Medical University, Kunming, Yunnan, 650032, China
[ 3 ] [Nie, Z.]Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China
[ 4 ] [Nie, Z.]Kunming College of Life Science, University of the Chinese Academy of Sciences, Kunming, 650204, China
[ 5 ] [Jiang, X.]Medical Faculty of Kunming University of Science and Technology, Kunming, 650500, China
[ 6 ] [Ye, J.]College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 7 ] [Wei, Z.]Department of Pathology, Affiliated Hospital of Qingdao University, Qingdao, 266071, China
[ 8 ] [Cheng, D.]Department of Pathology, First Affiliated Hospital of Kunming Medical University, Kunming, Yunnan, 650032, China
[ 9 ] [Wang, C.]Department of Pathology, First Affiliated Hospital of Kunming Medical University, Kunming, Yunnan, 650032, China
[ 10 ] [Wu, Y.]Department of Pathology, First Affiliated Hospital of Kunming Medical University, Kunming, Yunnan, 650032, China
[ 11 ] [Wu, Y.]Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China
[ 12 ] [Wu, Y.]Kunming College of Life Science, University of the Chinese Academy of Sciences, Kunming, 650204, China
[ 13 ] [Liu, R.]Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China
[ 14 ] [Liu, R.]Translational Cancer Research Center, Peking University First Hospital, Beijing, 100034, China
[ 15 ] [Chen, H.]College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350116, China
[ 16 ] [Chen, C.]Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China
[ 17 ] [Chen, C.]KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China
[ 18 ] [Chen, C.]Institute of Translation Medicine, Shenzhen Second People's Hospital, First Affiliated Hospital of Shenzhen University, Shenzhen, 518035, China
[ 19 ] [Wang, C.]Department of Pathology, First Affiliated Hospital of Kunming Medical University, Kunming, Yunnan, 650032, China

Reprint 's Address：

[Wang, C.]Department of Pathology, First Affiliated Hospital of Kunming Medical University, Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of SciencesChina

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chunyan740729@sina.com

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ISSN： 1945-4589

Year： 2020

Issue： 10

Volume： 12

Page： 9621-9632

5 . 6 8 2

JCR@2020

3 . 9 0 0

JCR@2023

ESI HC Threshold：253

JCR Journal Grade：1

CAS Journal Grade：1

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SCOPUS Cited Count： 3

ESI Highly Cited Papers on the List： 0 Unfold All

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Chinese Cited Count：

30 Days PV： 1

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