PDF(Pubmed)
Abstract：
The properties of a cell are determined both genetically by the DNA sequence of its genes and epigenetically through processes that regulate the pattern, timing and magnitude of expression of its genes. While the genetic basis of disease has been a topic of intense study for decades, recent years have seen a dramatic increase in the understanding of epigenetic regulatory mechanisms and a growing appreciation that epigenetic misregulation makes a significant contribution to human disease. Several large protein families have been identified that act in different ways to control the expression of genes through epigenetic mechanisms. Many of these protein families are finally proving tractable for the development of small molecules that modulate their function and represent new target classes for drug discovery. Here, we provide an overview of some of the key epigenetic regulatory proteins and discuss progress towards the development of pharmacological tools for use in research and therapy.
摘要：
细胞的特性既由其基因的DNA序列在遗传上决定，也通过调节模式的过程在表观遗传学上决定，其基因表达的时间和幅度。虽然疾病的遗传基础几十年来一直是一个激烈研究的话题，近年来，人们对表观遗传调控机制的理解急剧增加，并且越来越认识到表观遗传失调对人类疾病有重要贡献。已经确定了几个大的蛋白质家族，它们以不同的方式通过表观遗传机制控制基因的表达。这些蛋白质家族中的许多最终被证明易于开发调节其功能并代表药物发现的新靶标类别的小分子。这里,我们概述了一些关键的表观遗传调控蛋白，并讨论了用于研究和治疗的药理学工具的开发进展。
