As a transcription factor with a wide range of roles, c-Myc is a key protein in the regulation of cell fate, but it is also recognized as one of the targets that are difficult to become a drug. Therefore, the regulation and intervention means of c-Myc has been one of the frontier and hotspot directions of international competition, and the relevant targeting research will receive wide attention and cause further breakthroughs in the field of stem cell, tumor and drug development once important progress is made.

Recently, a research team from the Institute of Military Medical Research, Chinese Academy of Military Science, published a paper entitled “A Functional Screening Identifies a New Organic Selenium Compound Targeting” in Advanced Science. A Functional Screening Identifies a New Organic Selenium Compound Targeting Cancer Stem Cells: Role of c-Myc Transcription Activity Inhibition in Liver Cancer”. The research team discovered and synthesized CU27, an organic selenium small molecule compound that can target c-Myc regulation.

The research team took a unique approach to find small molecules that inhibit cancer stem cell stemness in the library of independently synthesized lead compounds, and then verified whether they can target c-Myc protein expression through histological and pharmacological analyses. The researchers further analyzed and found that CU27 can bind to the structural domain of c-Myc protein, which in turn blocks the formation of the c-Myc-Max complex, thereby preventing the transcriptional regulatory activity of self-renewal mediated by the complex. Through functional comparisons, the team found that the stemness inhibitory activity of CU27 was 10-fold and 14-fold higher than that of the two commercial c-Myc inhibitors, respectively. Subsequently, the researchers further validated the therapeutic effect of CU27 in targeting hepatocellular carcinoma stem cells in animals using an experimental animal model.

In summary, the research team indicated that CU27 has important application prospects both for the establishment of a safe and efficient stem cell-induced differentiation system, as well as for the targeted treatment of diseases including tumors, radiation damage, inflammation, and other related diseases, and regeneration and repair of tissue damage.

　Source: China Biotechnology Development Center

Note: This research result is extracted from the journal Advanced Science, the content of the article does not represent the views and positions of this website, for reference only.