A natural product-like inhibitor of NEDD8-activating enzyme.
The natural product-like 6,6″-biapigenin has been identified as only the second inhibitor of NEDD8-activating enzyme using virtual screening. This compound was active in enzyme and cell-based assays, with potency in the micromolar range.
Centre for Cancer and Inflammation Research, School of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong Kong. duncanl@hkbu.edu.hk
Chung-Hang
CH
Leung
Daniel Shiu-Hin
DS
Chan
Hui
H
Yang
Ruben
R
Abagyan
Simon Ming-Yuen
SM
Lee
Guo-Yuan
GY
Zhu
Wang-Fun
WF
Fong
Dik-Lung
DL
Ma
D047310:Apigenin / Q000737:chemistry*; D044946:Biflavonoids / Q000737:chemistry*; D001665:Binding Sites; D045744:Cell Line, Tumor; D003198:Computer Simulation; D003517:Cyclopentanes / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D000075687:NEDD8 Protein; D011743:Pyrimidines / Q000737:chemistry; D014452:Ubiquitins / Q000037:antagonists & inhibitors* / Q000378:metabolism
D044946:Biflavonoids; D003517:Cyclopentanes; D000075687:NEDD8 Protein; C082860:NEDD8 protein, human; D011743:Pyrimidines; D014452:Ubiquitins; C446502:biapigenin; D047310:Apigenin; C539933:pevonedistat