Repression of the transcriptional activity of ERR α with sequence-specific DNA-binding polyamides

In this study, we evaluated the potential for a pyrrole-imidazole polyamide to block ERR α binding to ERREs to inhibit gene expression. We demonstrated that the ERRE-targeted polyamide 1 blocked the binding of ERRα to the consensus ERRE and reduced the transcriptional activity of ERRα in cell culture. We further showed that inhibiting ERRα transcriptional activity with polyamide 1 l ed to reduced mitochondrial oxygen consumption, a primary biological effect regulated by ERRα. Finally, our data demonstrated that polyamide 1 is an inhibitor for cancer cell growth.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research