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A short Nur77-derived peptide converts Bcl-2 from a protector to a killer
Kolluri, Siva Kumar ; Zhu, Xiuwen ; Zhou, Xin ; Lin, Bingzhen ; Chen, Ya ; Sun, Kai ; Tian, Xuefei ; Town, James ; Cao, Xihua ; Lin, Feng ; Zhai, Dayong ; Kitada, Shinichi ; Luciano, Frederick ; O'Donnell, Edmond ; Cao, Yu ; He, Feng ; Lin, Jialing ; Reed, John C. ; Satter ; Zhang XK(张晓坤)
刊名http://dx.doi.org/10.1016/j.ccr.2008.09.002
2008-10-07
关键词CELL-DEATH BH3-ONLY PROTEINS FAMILY PROTEINS BH3 DOMAIN MITOCHONDRIAL APOPTOSIS INDUCE APOPTOSIS FLEXIBLE LOOP SOLID TUMORS BAX ACTIVATION
英文摘要National Institutes of Health [CA109345, CA119785, GM060554, GM062964]; US Army Medical Research and Material Command [W81XWH-08-1-0478, DAMD17-03-1-0427]; California Tobacco-Related Diseases Research Program (CTRDRP) [11RT-0081]; California Breast Cancer; Bcl-2 can be converted into a proapoptotic molecule by nuclear receptor Nur77. However, the development of Bcl-2 converters as anticancer therapeutics has not been explored. Here we report the identification of a Nur77-derived Bcl-2-converting peptide with 9 amino acids (NuBCP-9) and its enantiomer, which induce apoptosis of cancer cells in vitro and in animals. The apoptotic effect of NuBCPs and their activation of Bax are not inhibited but rather potentiated by Bcl-2. NuBCP-9 and its enantiomer bind to the Bcl-2 loop, Which shares the characteristics of structurally adaptable regions with many cancer-associated and signaling proteins. NuBCP-9s act as molecular switches to dislodge the Bcl-2 BH4 domain, exposing its BH3 domain, which in turn blocks the activity of antiapoptotic Bcl-X-L.
语种英语
出版者CANCER CELL
内容类型期刊论文
源URL[http://dspace.xmu.edu.cn/handle/2288/93065]  
专题药学院-已发表论文
推荐引用方式
GB/T 7714
Kolluri, Siva Kumar,Zhu, Xiuwen,Zhou, Xin,et al. A short Nur77-derived peptide converts Bcl-2 from a protector to a killer[J]. http://dx.doi.org/10.1016/j.ccr.2008.09.002,2008.
APA Kolluri, Siva Kumar.,Zhu, Xiuwen.,Zhou, Xin.,Lin, Bingzhen.,Chen, Ya.,...&张晓坤.(2008).A short Nur77-derived peptide converts Bcl-2 from a protector to a killer.http://dx.doi.org/10.1016/j.ccr.2008.09.002.
MLA Kolluri, Siva Kumar,et al."A short Nur77-derived peptide converts Bcl-2 from a protector to a killer".http://dx.doi.org/10.1016/j.ccr.2008.09.002 (2008).
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