Analysis of a transcriptional regulatory mechanism by histone/p53 demethylase complex

本研究旨在分析人类染色质转录的调控机制。关于LSD 1，去甲基化核因子，如人类组蛋白H3和肿瘤抑制基因产物p53，我们解决了LSD 1晶体结构与小分子量抑制剂，以前已经确定了我们的小组。我们发现其中一个LSD 1抑制剂表现出良好的细胞渗透性，三个抑制剂表现出基因表达调节活性。

This study aimed to analyze a regulatory mechanism of human chromatin transcription. Pertaining to LSD1 that demethylates nuclear factors such as human histone H3 and tumor suppressor gene product p53, we solved LSD1 crystal structures in complex with small molecular weight inhibitors that had been previously identified by our group. We revealed that one of the LSD1 inhibitors showed good cell permeability and three of the inhibitors exhibited gene expression regulatory activities.