Mdm2
Mouse double minute 2 homolog (MDM2) also known as E3 ubiquitin-protein ligase Mdm2 is a protein that in humans is encoded by the MDM2 gene. Mdm2 is an important negative regulator of the p53 tumor suppressor. Mdm2 protein functions both as an E3 ubiquitin ligase that recognizes the N-terminal trans-activation domain (TAD) of the p53 tumor suppressor and an inhibitor of p53 transcriptional activation.
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SP 141是高亲和性MDM2抑制剂。
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NSC 66811是MDM2 拮抗剂。 NSC 66811 disrupts MDM2-p53 interaction。
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Nutlin-3是一种有效的,选择性Mdm2(p53的环指依赖性泛素蛋白连接酶)拮抗剂,无细胞试验中IC50为90 nM;可稳定p53缺陷细胞中的p73。
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RITA (NSC 652287)诱导DNA-蛋白质和DNA-DNA交联,检测不到DNA单链断裂,通过靶向作用于p53,也抑制MDM2-p53相互作用。
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Nutlin-3a是Nutlin-3的活性对映体,抑制p53/MDM2相互作用,IC50为90 nM。
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