【摘 要】
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Functional inhibition of the p53 tumor suppressor protein by its negative regulators MDM2 and MDMX,whose genes MDM2 and MDMX are often amplified and/or over-expressed in many tumors harboring wild typ
【机 构】
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Institute of Human Virology and Department of Biochemistry and Molecular Biology,University of Maryl
【出 处】
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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Functional inhibition of the p53 tumor suppressor protein by its negative regulators MDM2 and MDMX,whose genes MDM2 and MDMX are often amplified and/or over-expressed in many tumors harboring wild type TP53,directly contributes to tumor development and progression.MDM2 is an E3 ubiquitin ligase that specifically targets p53 for proteosomal degradation-a process potentiated by MDM2 hetero-oligomerization with its homolog MDMX.Both MDM2 and MDMX can also antagonize p53 transcription activity by sequestering p53 transactivation domain via their N-terminal p53-binding domains.Disrupting the p53-MDM2/MDMX inhibitory complex to rescue p53 function has been validated as a viable therapeutic strategy for cancer treatment.
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