Integrated virtual screening and MD simulation approaches toward discovering potential inhibitors for targeting BRPF1 bromodomain in hepatocellular carcinoma

Uncovering the non-histone interactome of the BRPF1 bromodomain using site-specific azide-acetyllysine photochemistry

“…Like other bromodomain-containing proteins, BRPF1 too is involved in various cellular processes like skeletal development, vertebrate segmentation and patterning, brain development and even in cancer-like hepatocellular carcinoma (HCC) ( 12 , 32 ). In HCC, it was shown that BRPF1 was among the most significantly upregulated bromodomain-containing protein and its expression negatively correlates with patients’ survival ( 32 , 33 ). Moreover, inhibition of BRPF1 by CRISPR KO or treatment with BRPF1 bromodomain specific inhibitor GSK5959 inhibited HCC growth in vivo demonstrating that BRPF1s′ bromodomain specific functions are essential determinants of HCC tumorigenesis ( 32 ).…”