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Identification of RIP1 kinase as a specific cellular target of necrostatins
文献类型：期刊论文
| 作者 | Alexei Degterev ; Junichi Hitomi ; Megan Germscheid ; Irene L Ch'en ; Olga Korkina ; Xin Teng ; Derek Abbott ; Gregory D. Cuny ; Yuan CY(袁承业) ; Gerhard Wagner ; Stephen M. Hedrick ; Scott A. Gerber ; Alexey Lugovskoy ; Yuan JY(袁钧瑛) |
| 刊名 | Nat. Chem. Biol.
 |
| 出版日期 | 2008 |
| 卷号 | 4期号:5页码:313-321 |
| ISSN号 | 1552-4450 |
| 其他题名 | R1P1 激酶是NECROSTATINS抑制剂的特殊细胞靶点的鉴定证明 |
| 英文摘要 | Necroptosis is a cellular mechanism of necrotic cell death induced by apoptotic stimuli in the form of death domain receptor engagement by their respective ligands under conditions where apoptotic execution is prevented. Although it occurs under regulated conditions, necroptotic cell death is characterized by the same morphological features as unregulated necrotic death. Here we report that necrostatin-1, a previously identified small-molecule inhibitor of necroptosis, is a selective allosteric inhibitor of the death domain receptor-associated adaptor kinase RIP1 in vitro. We show that RIP1 is the primary cellular target responsible for the antinecroptosis activity of necrostatin-1. In addition, we show that two other necrostatins, necrostatin-3 and necrostatin-5, also target the RIP1 kinase step in the necroptosis pathway, but through mechanisms distinct from that of necrostatin-1. Overall, our data establish necrostatins as the first-in-class inhibitors of RIP1 kinase, the key upstream kinase involved in the activation of necroptosis. |
| 学科主题 | 生命有机化学 |
| 收录类别 | SCI |
| 原文出处 | http://dx.doi.org/10.1038/nchembio.83 |
| 语种 | 英语 |
| WOS记录号 | WOS:000255170400012 |
| 公开日期 | 2013-01-09 |
| 源URL | [http://202.127.28.38/handle/331003/11072]  |
| 专题 | 上海有机化学研究所_上海有机化学研究所 |
| 推荐引用方式 GB/T 7714 | Alexei Degterev,Junichi Hitomi,Megan Germscheid,et al. Identification of RIP1 kinase as a specific cellular target of necrostatins[J]. Nat. Chem. Biol.,2008,4(5):313-321. |
| APA | Alexei Degterev.,Junichi Hitomi.,Megan Germscheid.,Irene L Ch'en.,Olga Korkina.,...&袁钧瑛.(2008).Identification of RIP1 kinase as a specific cellular target of necrostatins.Nat. Chem. Biol.,4(5),313-321. |
| MLA | Alexei Degterev,et al."Identification of RIP1 kinase as a specific cellular target of necrostatins".Nat. Chem. Biol. 4.5(2008):313-321. |
入库方式： OAI收割
来源：上海有机化学研究所
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