Progress in the researches for antitumor NEDD8 activating enzyme inhibitors

GUO Yahui; LU Peng; WANG Yubin; ZHANG Huibin

doi:10.11665/j.issn.1000-5048.20170603

Journal of China Pharmaceutical University > 2017 > 48(6): 646-653. > DOI: 10.11665/j.issn.1000-5048.20170603

GUO Yahui, LU Peng, WANG Yubin, ZHANG Huibin. Progress in the researches for antitumor NEDD8 activating enzyme inhibitors[J]. Journal of China Pharmaceutical University, 2017, 48(6): 646-653. DOI: 10.11665/j.issn.1000-5048.20170603

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Progress in the researches for antitumor NEDD8 activating enzyme inhibitors

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Abstract

Inhibition of NEDD8 activating enzyme(NAE), the rate limiting enzyme in Neddylation, can suppress the activity of ubiquitin-proteasome system(UPS)pathway and decrease degradations of related proteins, resulting in cell apoptosis. Compared with the proteasome inhibitors, NAE inhibitors can interfere with cellular homeostasis with more specificity. With the rapid development of the research on NAE, a variety of NAE inhibitors have been reported. According to the structure characteristics, NAE inhibitors can be divided into the AMP analogues, double flavonoids deoxidization duckbill alkali ketone derivatives and metal rhodium complex classes, etc. The process of ubiquitinated modified Neddylation, NAE and physiological role of tumor has been introduced in this paper, and the latest progress of NAE inhibitors also has been summarized.
- NEDD8 activating enzyme,
- inhibitors,
- antitumor,
- advances

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