Pushpavalli, S.N., Janaki Ramaiah, M., Lavanya, A., Raksha Ganesh, A., Kumbhare, R.M., Bhadra, K., Bhadra, U., Pal-Bhadra, M. (2012). Imidazo-benzothiazoles a potent microRNA modulator involved in cell proliferation.  Bioorg. Med. Chem. Lett. 22(20): 6418--6424.

FBrf0219513

Research paper

MicroRNAs are endogenously expressed tiny non-coding RNAs that control gene expression at the post-transcriptional level and regulate processes of cell growth, differentiation, proliferation and apoptosis. Aberrant expression of microRNAs correlates with various cancers. Our experiments demonstrated that imidazo-benzothiazole conjugates caused apoptosis in colon cancer cells by modulating the expression of microRNAs. In vivo study in Drosophila melanogaster has exhibited inhibitory action on bantam microRNA, the homolog of human miR-542-5p that is involved in deciding the cellular cues that regulate the balance between proliferation and apoptosis. The expression of direct targets of bantam such as Hid and HDAC-6 were affected upon compound treatment. Interestingly, these conjugates downregulate the genes involved in microRNA biogenesis such as Drosha, Pasha and Dicer-1. Our findings have elucidated the microRNA inhibitory role of imidazo-benzothiazole conjugates.