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Identification of RIP1 kinase as a specific cellular target of necrostatins
其他题名R1P1 激酶是NECROSTATINS抑制剂的特殊细胞靶点的鉴定证明
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)
2008
发表期刊Nat. Chem. Biol.
ISSN1552-4450
卷号4期号:5页码:313-321
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.
学科领域生命有机化学
部门归属Tufts Univ; Harvard Univ; Univ Calif San Diego; Harvard Univ; Brigham & Womens Hosp; Beth Israel Deaconess Med Ctr; 上海有机所; Norris Cotton Canc Ctr; Dartmouth Med Sch
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收录类别SCI
语种英语
WOS记录号WOS:000255170400012
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文献类型期刊论文
条目标识符http://ir.sioc.ac.cn/handle/331003/11072
专题上海有机化学研究所
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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.
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