GSE109870 transcriptome studies of BRD4 inhibitor BDF-1253 on renal clear carcinoma 786-O cells

In this study, a novel category of BRD4 inhibitors, which are originated from an approved drug Nitroxoline and its analogues, were synthesized and evaluated by biochemical and cellular assays, as well as the method of crystallography and xenograft mice models. In renal cell carcinoma cell lines, these compounds exhibited efficient inhibition against the expression and protein abundance of BRD4 downstream genes. Moreover, the complex crystal structures of several compounds in this series with the first bromodomain of BRD4 were solved, which revealed the binding mechanism of this novel category of BRD4 inhibitors and facilitated further structural modifications. This series of novel BRD4 inhibitors is promising to become drug candidates for the treatment of renal cell carcinoma after further development and assessments.
Source: GEO: Gene Expression Omnibus - Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Homo sapiens Source Type: research