Ursolic acid derivative FZU-03,010 inhibits STAT3 and induces cell cycle arrest and apoptosis in renal and breast cancer cells - Details

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Abstract：

Advanced　renal　cell　carcinoma　and　triple　negative　breast　cancer　(TNBC)　are　malignancies　without　effective　therapeutics　currently.　Ursolic　acid　(UA)　has　been　previously　reported　to　have　anti-cancer　effects　in　multiple　solid　tumors.　In　order　to　develop　more　potent　anti-cancer　reagents,　FZU-03,010　based　on　the　chemical　structure　of　UA　were　synthesized.　The　results　demonstrated　that,　compared　with　UA,　FZU-03,010　could　suppress　renal　cancer　cell　786-0　and　TNBC　cell　HCC1806　cell　viability　more　potently.　Furthermore,　FZU-03,010　could　induce　G1　cell　cycle　arrest　and　cell　apoptosis　more　efficiently　than　UA.　FZU-03,010　could　also　inhibit　signal　transducer　and　activator　of　transcription　3　activation,　induce　the　expression　of　cell　cycle-dependent　kinase　inhibitors　(p21　and　p27)　and　promote　cell　apoptosis.　In　conclusion,　our　results　suggest　that　the　UA　derivative　FZU-03,010　is　more　potent　in　inhibiting　cancer　cell　survival,　and　FZU-03,010　has　the　potential　to　be　developed　as　a　therapeutic　for　renal　cell　cancers　and　TNBCs.　©　The　Author　2017.　Published　by　Oxford　University　Press　on　behalf　of　the　Institute　of　Biochemistry　and　Cell　Biology,　Shanghai　Institutes　for　Biological　Sciences,　Chinese　Academy　of　Sciences.　All　rights　reserved.

Keyword：

FZU-03; Renal cell carcinoma; STAT3; Triple negative breast cancer; Ursolic acid

Community：

[ 1 ] [Li, W.]Department of Urology, First People's Hospital of Yunnan Province, Kunming, 650032, China
[ 2 ] [Li, W.]Medical College of Kunming University of Science and Technology, Kunming, 650032, China
[ 3 ] [Zhang, H.]Department of Urology, First People's Hospital of Yunnan Province, Kunming, 650032, China
[ 4 ] [Zhang, H.]Medical College of Kunming University of Science and Technology, Kunming, 650032, China
[ 5 ] [Nie, M.]Department of Urology, First People's Hospital of Yunnan Province, Kunming, 650032, China
[ 6 ] [Nie, M.]Medical College of Kunming University of Science and Technology, Kunming, 650032, China
[ 7 ] [Tian, Y.]Department of Urology, First People's Hospital of Yunnan Province, Kunming, 650032, China
[ 8 ] [Tian, Y.]Yunnan University of Traditional Chinese Medicine, Kunming, 650032, China
[ 9 ] [Chen, X.]Department of Urology, First People's Hospital of Yunnan Province, Kunming, 650032, China
[ 10 ] [Chen, X.]Medical College of Kunming University of Science and Technology, Kunming, 650032, China
[ 11 ] [Chen, C.]Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China
[ 12 ] [Chen, H.]College of Chemistry, Fuzhou University, Fuzhou, 350116, China
[ 13 ] [Liu, R.]Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, China

Reprint 's Address：

[Liu, R.]Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of SciencesChina

Email：

liurong@mail.kiz.ac.cn

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Source ：

Acta Biochimica et Biophysica Sinica

ISSN： 1672-9145

Year： 2017

Issue： 4

Volume： 49

Page： 367-373

2 . 2 2 4

JCR@2017

3 . 3 0 0

JCR@2023

ESI HC Threshold：231

JCR Journal Grade：3

CAS Journal Grade：4

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WoS CC Cited Count：

SCOPUS Cited Count： 27

ESI Highly Cited Papers on the List： 0 Unfold All

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Chinese Cited Count：

30 Days PV： 0

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