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.
1.Chinese Acad Sci, Guangzhou Inst Biomed, Div Mol Carcinogenesis & Targeted Therapy Canc, Beijing, Peoples R China 2.Chinese Acad Sci, Guangzhou Inst Hlth, Div Mol Carcinogenesis & Targeted Therapy Canc, Beijing, Peoples R China 3.Chinese Acad Sci, State Key Lab Biomembrane & Membrane Biotechnol, Inst Zool, Beijing, Peoples R China 4.Univ Sci & Technol China, Hefei 230026, Peoples R China 5.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming, Peoples R China 6.Nanfang Med Univ, Nanfang Hosp, Dept Hematol, Guangzhou, Guangdong, Peoples R China
Liu, Jing-Lei,Zeng, Guang-Zhi,Liu, Xiao-Li,et al. Small compound bigelovin exerts inhibitory effects and triggers proteolysis of E2F1 in multiple myeloma cells[J]. CANCER SCIENCE,2013,104(12):1697-1704.