Bromodomain小分子抑制剂的研究进展

Progress in the Research of Small Molecule Inhibitors of Bromodomains

草甘膦是一种高效、低毒的灭生性除草剂,在世界范围内得到广泛应用。本文概述了IDA法和甘氨酸法草甘膦母液的主要成分,总结了草甘膦的主要回收方法,指出了现有研究的不足之处,为进一步研究提供参考。

ε-N-acetylation of lysine residues on histone tails is one of the most important post-translational modification states in the human proteome. Bromodomains (BRDs) are the only interaction modules that specifically recognize Kac. Histone aceyl-transferases, BRDs and Histone deactylases form a system of 'write-read-erase', which has been linked with the transfer of epigenetic information. Over the past decade, the great attention has been paid to the potent and selective small molecule inhibitors targeting at BRDs. Herein, this review is focused on the discoveries, modes of action, biological activities, synthetic methods and the SAR of the small molecular BRD inhibitors to date.