【摘 要】
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SUMO(small ubiquitin-related modifier) was found to conjugate with a number of proteins to regulate cellular functions including transcription,signal transduction,and cell cycle.SUMO-specific protease
【机 构】
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School of Pharmacy,Shanghai Jiao Tong University,Shanghai 200240
【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
SUMO(small ubiquitin-related modifier) was found to conjugate with a number of proteins to regulate cellular functions including transcription,signal transduction,and cell cycle.SUMO-specific proteases(SENPs) reversibly remove SUMO from the SUMOylated proteins.Recently,SENP 1 was found to be a potential therapeutic target for the treatment of prostate cancers.We designed and synthesized a series of benzodiazepine-based SENP1 inhibitors,and they showed inhibitory activity as good as IC50=3.9 μM.These inhibitors could serve as potential anticancer agents as well as chemical probes in the understanding of the biological roles of SENP1.
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