1345046-75-4Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of benzodiazepine-based SUMO-specific protease 1 inhibitors
Qiao, Zhitao,Wang, Weiwei,Wang, Lie,Wen, Donghua,Zhao, Yaxue,Wang, Qing,Meng, Qingqing,Chen, Guoqiang,Wu, Yingli,Zhou, Huchen
, p. 6389 - 6392 (2011)
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 removeSUMOfrom 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 benzodiazepinebased SENP1 inhibitors, and they showed inhibitory activity as good as IC50 = 9.2 μM (compound 38). The structure-activity relationship was also discussed.
