Peng, Ting; He, Yujiao; Wang, Tao; Yu, Jialing; Ma, Xiaofang; Zhou, Zongyuan; Sheng, Yuwen; Li, Lingyu; Peng, Huipan; Li, Sheng; Zou, Jiawei; Yuan, Yi; Zhao, Yongyun; Shi, Hailong; Li, Fu; Liu, Wanli; Hu, Kaifeng; Lu, Xiaoxia; Zhang, Guolin; Wang, Fei published the artcile< Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis>, Reference of 3959-07-7, the main research area is hepatocellular carcinoma miRNA biogenesis TRBP SAR proliferation cancer therapy.
MicroRNAs (miRNAs) are key players in human hepatocellular carcinoma (HCC) tumorigenesis. Therefore, small mols. targeting components of miRNA biogenesis may provide new therapeutic means for HCC treatment. By a high-throughput screening and structural simplification, we identified a small mol., CIB-3b (I), which suppresses the growth and metastasis of HCC in vitro and in vivo by modulating expression profiles of miRNAome and proteome in HCC cells. Mechanistically, CIB-3b phys. binds to transactivation response (TAR) RNA-binding protein 2 (TRBP) and disrupts the TRBP-Dicer interaction, thereby altering the activity of Dicer and mature miRNA production Structure-activity relationship study via the synthesis of 45 CIB-3b derivatives showed that some compounds exhibited a similar inhibitory effect on miRNA biogenesis to CIB-3b. These results support TRBP as a potential therapeutic target in HCC and warrant further development of CIB-3b along with its analogs as a novel therapeutic strategy for the treatment of HCC.
Journal of Medicinal Chemistry published new progress about A-kinase anchor protein 10 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Reference of 3959-07-7.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary