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学科主题: 药学
题名:
Anticancer Effect of a Novel Proteasome Inhibitor, YSY01A, via G2/M Arrest in PC-3M Cells in vitro and in vivo
作者: Zhang, Mei1,3; Yuan, Xia1; Xu, Bo1; Guo, Wei1; Ran, Fu-Xiang1; Li, Run-Tao2; Cui, Jing-Rong1
关键词: Anticancer ; proteasome inhibitor ; tripeptideboronic acid ; PC-3M cell ; cell cycle
刊名: JOURNAL OF CANCER
发表日期: 2015
DOI: 10.7150/jca.11785
卷: 6, 期:8, 页:701-708
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Oncology
研究领域[WOS]: Oncology
关键词[WOS]: INDEPENDENT PROSTATE-CANCER ; ADVANCED SOLID TUMORS ; PHASE-II TRIAL ; MULTIPLE-MYELOMA ; HUMAN P53 ; BORTEZOMIB ; APOPTOSIS ; UBIQUITIN ; TRANSITION ; RESISTANCE
英文摘要:

YSY01A is a new tripeptideboronic acid and an analog of PS341. However, YSY01A′s antitumor effects and mechanism have not yet been elucidated. This study demonstrates that YSY01A inhibited proteasome activity by combining with the chymotrypsin-like (CT-L) site (beta 5i/beta 5), the post-glutamyl peptide hydrolase (PGPH) site (beta 1i/beta 1) and the trypsin-like (T-L) site (beta 2i/beta 2) in special fluorgonic substrates and proteasome probe tests. We explored the anticancer effect using methyl thiazolyltetrazolium (MTT) or sulforhodamine B (SRB), and PC-3M cells were sensitive to YSY01A among the four cancer cell types tested. The YSY01A antiproliferative effect was stronger than that of PS341. In vivo, YSY01A (1.25, 2.25, and 3.25 mg/kg) inhibited PC-3M cell xenograft tumor growth, and the tumor volume inhibition rate was approximately 40% to 60%. YSY01A arrested PC-3M cells in the G2/M phase of the cell cycle by flow cytometry (FCM). Many proteins related to the cell cycle were analyzed using western blot, and YSY01A was shown to increase p21, p27, cyclinB1, P-cdc2 (tyr15) and wee1 protein expression in both cells and tumor tissue in a concentration-dependent manner. YSY01A, a proteasome inhibitor, exerts anticancer effects on PC-3M cells in vitro and in vivo. The mechanism of the YSY01A-mediated antitumor effect is that the cell cycle is arrested at the G2/M stage. This study suggests that YSY01A may be a novel therapeutic agent for prostate cancer.

语种: 英语
所属项目编号: 2009ZX0930010 ; 81172915 ; 2009ZX09301010
项目资助者: Eleventh Five Year Plan for National Science and Technology Major Project ; National Natural Science Foundation of China ; Major New Drugs Research and Development Platform of Peking University
WOS记录号: WOS:000360298200003
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59789
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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作者单位: 1.State Key Lab Nat & Biomimet Drugs, Beijing, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
3.Shihezi Univ, Sch Pharmaceut Sci, Dept Pharmacol, Xinjiang 832000, Peoples R China

Recommended Citation:
Zhang, Mei,Yuan, Xia,Xu, Bo,et al. Anticancer Effect of a Novel Proteasome Inhibitor, YSY01A, via G2/M Arrest in PC-3M Cells in vitro and in vivo[J]. JOURNAL OF CANCER,2015,6(8):701-708.
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