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Anticancer Effect of a Novel Proteasome Inhibitor, YSY01A, via G2/M Arrest in PC-3M Cells in vitro and in vivo
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
2015
DOI10.7150/jca.11785
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
WOS记录号WOS:000360298200003
引用统计
被引频次:3[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/59789
专题北京大学临床肿瘤学院_肿瘤放疗科
北京大学药学院_天然药物与仿生药物国家重点实验室
北京大学药学院_化学生物学系
北京大学药学院_分子与细胞药理学系
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
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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.
APA Zhang, Mei.,Yuan, Xia.,Xu, Bo.,Guo, Wei.,Ran, Fu-Xiang.,...&Cui, Jing-Rong.(2015).Anticancer Effect of a Novel Proteasome Inhibitor, YSY01A, via G2/M Arrest in PC-3M Cells in vitro and in vivo.JOURNAL OF CANCER,6(8),701-708.
MLA Zhang, Mei,et al."Anticancer Effect of a Novel Proteasome Inhibitor, YSY01A, via G2/M Arrest in PC-3M Cells in vitro and in vivo".JOURNAL OF CANCER 6.8(2015):701-708.
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