AI Article Synopsis
- The study focuses on the role of estrogen-related receptors (ERRs) in regulating cellular metabolism and cancer growth by binding to specific DNA elements called ERREs.
- Researchers tested a compound, pyrrole-imidazole polyamide, to see if it could block ERRα from binding to these elements and thus inhibit gene expression.
- Results showed that this compound effectively reduced ERRα's transcriptional activity, leading to decreased mitochondrial oxygen consumption and inhibiting cancer cell growth.
Article Abstract
The orphan nuclear receptors estrogen-related receptors (ERRs) bind to the estrogen-related receptor response element (ERRE) to regulate transcriptional programs in cellular metabolism and cancer cell growth. In this study, we evaluated the potential for a pyrrole-imidazole polyamide to block ERRα 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 led 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.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8455084 | PMC |
| http://dx.doi.org/10.1007/s00044-019-02493-4 | DOI Listing |
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