ATAD2 (ANCCA) is an epigenetic regulator and transcriptional cofactor, whose overexpression has been linked to the progress of various cancer types. Here, we report a DNA-encoded library screen leading to the discovery of BAY-850, a potent and isoform selective inhibitor that specifically induces ATAD2 bromodomain dimerization and prevents interactions with acetylated histones in vitro, as well as with chromatin in cells. These features qualify BAY-850 as a chemical probe to explore ATAD2 biology.

中文翻译：

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具有新型化学结构和异常作用方式的同工型选择性ATAD2化学探针

ATAD2（ANCCA）是一种表观遗传调控因子和转录辅助因子，其过表达与各种癌症类型的进展有关。在这里，我们报告了一种DNA编码的文库筛选，导致发现了BAY-850，这是一种有效且同种型的选择性抑制剂，可特异性诱导ATAD2溴结构域二聚化并阻止与乙酰化组蛋白的体外相互作用以及与细胞中的染色质的相互作用。这些功能使BAY-850成为探索ATAD2生物学的化学探针。