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ID: ALA1909559
Journal: Bioorg Med Chem Lett
Title: Design, synthesis, and biological evaluation of benzodiazepine-based SUMO-specific protease 1 inhibitors.
Authors: Qiao Z, Wang W, Wang L, Wen D, Zhao Y, Wang Q, Meng Q, Chen G, Wu Y, Zhou H.
Abstract: As the best-characterized ubiquitin-like protein (UBL), small ubiquitin-related modifier (SUMO) was found to conjugate with a number of proteins to regulate cellular functions including transcription, signal transduction, and cell cycle. While E1, E2 and E3 ligases are responsible for the forward SUMOylation reaction, SUMO-specific proteases (SENPs) reversibly remove SUMO from the SUMOylated proteins. Recently, SENP1 was found to be a potential therapeutic target for the treatment of prostate cancers, but the design and synthesis of its inhibitors have not been reported. We designed and synthesized a series of benzodiazepine-based SENP1 inhibitors, and they showed inhibitory activity as good as IC(50)=9.2μM (compound 38). The structure-activity relationship was also discussed.
CiteXplore: 21930380