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Small-molecule targeting of e3 ligase adaptor spop in kidney cancer

文献类型：期刊论文

作者Guo, Zhong-Qiang1,3,4; Zheng, Tong2,5; Chen, Baoen2; Luo, Cheng6; Ouyang, Sisheng6; Gong, Shouzhe2; Li, Jiafei2; Mao, Liu-Liang7; Lian, Fulin8; Yang, Yong9
刊名Cancer cell
出版日期2016-09-12
卷号30期号:3页码:474-484
ISSN号1535-6108
DOI10.1016/j.ccell.2016.08.003
通讯作者Yang, cai-guang(yangcg@simm.ac.cn) ; Liu, jiang(liuj@big.ac.cn) ; Jiang, hualiang(hljiang@simm.ac.cn)
英文摘要In the cytoplasm of virtually all clear-cell renal cell carcinoma (ccrcc), speckle-type poz protein (spop) is overexpressed and misallocated, which may induce proliferation and promote kidney tumorigenesis. in normal cells, however, spop is located in the nucleus and induces apoptosis. here we show that a structure-based design and subsequent hit optimization yield small molecules that can inhibit the spop-substrate protein interaction and can suppress oncogenic spop-signaling pathways. these inhibitors kill human ccrcc cells that are dependent on oncogenic cytoplasmic spop. notably, these inhibitors minimally affect the viability of other cells in which spop is not accumulated in the cytoplasm. our findings validate the spop-substrate protein interaction as an attractive target specific to ccrcc that may yield novel drug discovery efforts.
WOS关键词UBIQUITIN-PROTEASOME PATHWAY ; RENAL-CELL CARCINOMA ; PROSTATE-CANCER ; CLINICAL-TRIALS ; PROTEIN ; INHIBITORS ; INACTIVATION ; DEGRADATION ; SPECIFICITY ; COMPLEX
WOS研究方向Oncology ; Cell Biology
WOS类目Oncology ; Cell Biology
语种英语
出版者CELL PRESS
WOS记录号WOS:000383314200012
URI标识http://www.irgrid.ac.cn/handle/1471x/2376307
专题中国科学院大学
通讯作者Yang, Cai-Guang; Liu, Jiang; Jiang, Hualiang
作者单位1.Chinese Acad Sci, Beijing Inst Genom, CAS Key Lab Genome Sci & Informat, Beijing 100101, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Biol Chem Lab, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Peking Univ, Dept Urol, Hosp 1, Beijing 100034, Peoples R China
4.Wuhan Univ, Dept Urol, Zhongnan Hosp, Wuhan 430071, Hubei, Peoples R China
5.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
6.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China
7.Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China
8.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Analyt Chem, Shanghai 201203, Peoples R China
9.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
10.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Safety Evaluat & Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Guo, Zhong-Qiang,Zheng, Tong,Chen, Baoen,et al. Small-molecule targeting of e3 ligase adaptor spop in kidney cancer[J]. Cancer cell,2016,30(3):474-484.
APA Guo, Zhong-Qiang.,Zheng, Tong.,Chen, Baoen.,Luo, Cheng.,Ouyang, Sisheng.,...&Jiang, Hualiang.(2016).Small-molecule targeting of e3 ligase adaptor spop in kidney cancer.Cancer cell,30(3),474-484.
MLA Guo, Zhong-Qiang,et al."Small-molecule targeting of e3 ligase adaptor spop in kidney cancer".Cancer cell 30.3(2016):474-484.

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来源：中国科学院大学

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