Description
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein, disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). It is a coumarin-derived small molecule. CMLD-2 induces apoptosis and exhibits antitumor activity in different cancer cells, such as colon, pancreatic, thyroid and lung cancer cell lines. These biological effects of CMLD-2 could be due to the reduced stability of HuR mRNA targets involved in proliferative and anti-apoptotic pathways. Hu antigen R (HuR) is an RNA-binding protein that can regulate target mRNA stability and translation[1].
in vitro
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein, disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). It is a coumarin-derived small molecule. CMLD-2 induces apoptosis and exhibits antitumor activity in different cancer cells, such as colon, pancreatic, thyroid and lung cancer cell lines. These biological effects of CMLD-2 could be due to the reduced stability of HuR mRNA targets involved in proliferative and anti-apoptotic pathways. Hu antigen R (HuR) is an RNA-binding protein that can regulate target mRNA stability and translation.
References
[1] Lorenzo Allegri. “The HuR CMLD-2 inhibitor exhibits antitumor effects via MAD2 downregulation in thyroid cancer cells.” ACS Applied Electronic Materials (2019): 7374.