BRD8 inhibitor

BRD8 inhibitors are small molecule probes that selectively target the bromodomain-containing protein 8 (BRD8), specifically the first bromodomain (BD1). BRD8 is a subunit of the NuA4/TIP60 histone acetyltransferase complex and acts as an epigenetic reader of acetylated lysine residues. These inhibitors, including the probes DN01 and DN02, are being investigated for their ability to disrupt BRD8-mediated epigenetic regulation in various cancers. In TP53-wild-type glioblastoma, BRD8 has been identified as a key dependency that suppresses p53-mediated tumor suppression by recruiting the histone variant H2AZ to p53 target genes. Pharmacological inhibition of BRD8 displaces H2AZ, increases chromatin accessibility, and restores p53 transcriptional activity, leading to cell-cycle arrest and suppressed tumor growth. Beyond glioblastoma, BRD8 inhibitors are also being explored in colorectal and hepatocellular carcinomas.

Other names

BRD8 inhibitorsBRD-8 inhibitorsBRD 8 inhibitorsBRD8(BD1) inhibitors