BPTF (bromodomain and PHD finger containing transcription factor) is a multidomain protein that plays essential roles in transcriptional regulation, T-cell homeostasis and stem cell pluripotency. As part of the chromatin remodeling complex hNURF (nucleosome remodeling factor), BPTF epigenetic reader subunits are particularly important for BPTF cellular function. Here we report the synthesis of NVS-BPTF-1, a previously reported highly potent and selective BPTF-bromodomain inhibitor. Evaluation of the impact of the inhibition of BPTF-bromodomain using NVS-BPTF-1 on selected proteins involved in the antigen processing pathway revealed that exclusively targeting BPTF-bromodomain is insufficient to observe an increase of PSMB8, PSMB9, TAP1 and TAP2 proteins.

BPTF（含溴结构域和 PHD 指的转录因子）是一种多结构域蛋白，在转录调控、T细胞稳态和干细胞多能性中起重要作用。作为染色质重塑复合物 hNURF（核小体重塑因子）的一部分，BPTF 表观遗传阅读器亚基对 BPTF 细胞功能尤为重要。在这里，我们报告了 NVS-BPTF-1 的合成，这是一种先前报道的高效和选择性 BPTF-溴结构域抑制剂。使用 NVS-BPTF-1 对 BPTF-溴结构域的抑制对参与抗原加工途径的选定蛋白质的影响的评估表明，仅针对 BPTF-溴结构域不足以观察到 PSMB8、PSMB9、TAP1 和 TAP2 蛋白的增加。