Laboratory of Immune Cell Epigenetics and Signaling, The Rockefeller University, New York, New York 10065.
Cold Spring Harb Perspect Biol. 2014 Jun 2;6(6):a018671. doi: 10.1101/cshperspect.a018671.
Inflammation is associated with the activation of genes that contribute to immune defense and tissue repair. The bromodomain-containing proteins of the BET family, which recognize histone lysine acetylation, play a key role in the transcriptional control of inflammatory genes. Inhibition of BET proteins by the small-molecule inhibitor I-BET affects the expression of a particular subset of inflammatory genes-namely, ones that follow an "analog-like," but not "digital-like" activation pattern. This ability of I-BET to target genes based on the dynamic pattern of their activation may facilitate the further development of anti-inflammatory treatment protocols that are tuned to the individual or to disease-specific patterns of gene expression.
炎症与参与免疫防御和组织修复的基因激活有关。BET 家族含溴结构域的蛋白可识别组蛋白赖氨酸乙酰化,在炎症基因的转录控制中发挥关键作用。小分子抑制剂 I-BET 通过抑制 BET 蛋白,影响特定亚类炎症基因的表达,即遵循“类似模拟”而非“数字式”激活模式的基因。I-BET 基于基因激活的动态模式靶向基因的这种能力,可能有助于进一步开发针对个体或疾病特异性基因表达模式的抗炎治疗方案。