Related Experiment Video
Updated: May 7, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Small compound bigelovin exerts inhibitory effects and triggers proteolysis of E2F1 in multiple myeloma cells
Jing-Lei Liu1, Guang-Zhi Zeng, Xiao-Li Liu
1Division of Molecular Carcinogenesis and Targeted Therapy for Cancer, Guangzhou Institutes of Biomedicine and Health & State Key Laboratory of Biomembrane and Membrane Biotechnology, Institute of Zoology, Chinese Academy of Sciences, Beijing, China; University of Science and Technology of China, Hefei, China.
Abstract:
Multiple myeloma (MM) is a currently incurable blood cancer. Here we tested the effects of a small compound bigelovin on MM cells, and reported that it caused cell cycle arrest and subsequently induced apoptosis. Bigelovin triggered proteolysis of E2F1, which could be inhibited by caspase inhibitor. To investigate the clinical relevance, the expression of E2F1 in MM specimens was tested, and the results showed that E2F1 was overexpressed in 25-57% of MM patients and was associated with higher International Staging System (ISS) stage. These results suggest that E2F1 may be important for MM pathogenesis, and bigelovin could serve as a lead compound for the development of E2F1 inhibitor.
Related Concept Videos
Eukaryotic Transcription Inhibitors
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
Mitogens and the Cell Cycle
Inhibition of Cdk Activity
Inhibition of CDK Activity
Inhibitors of Bacterial Protein Synthesis
Abnormal Proliferation

