【摘要】：BET(bromodomain and extraterminal)是一類能解讀表觀遺傳密碼的蛋白,通過識(shí)別和結(jié)合乙�；慕M蛋白或非組蛋白,在調(diào)節(jié)基因轉(zhuǎn)錄中發(fā)揮重要的作用。BET抑制劑在腫瘤和炎癥等臨床前疾病模型中表現(xiàn)出良好的療效,且已有部分抑制劑進(jìn)入臨床階段,這表明以BET為治療靶點(diǎn)的藥物研發(fā)具有可觀前景。本文將對(duì)BET蛋白的結(jié)構(gòu)功能、BET抑制劑與疾病治療以及其作為治療靶點(diǎn)的分子機(jī)制等方面進(jìn)行闡述。
[Abstract]:BET (bromodomain and extraterminal) is a class of proteins that can interpret epigenetic codes by recognizing and binding acetylated histone or non-histone. BET inhibitors play an important role in regulating gene transcription. BET inhibitors have shown good efficacy in preclinical disease models such as tumor and inflammation, and some inhibitors have entered the clinical stage. This suggests that drug development with BET as a therapeutic target has a promising future. In this paper, the structure and function of BET protein, its inhibitor and disease treatment, and its molecular mechanism as therapeutic targets are reviewed.
【作者單位】： 美國伊利諾伊大學(xué)香檳分校生化系;中國醫(yī)學(xué)科學(xué)院北京協(xié)和醫(yī)學(xué)院醫(yī)藥生物技術(shù)研究所;
【基金】：基金項(xiàng)目:中國醫(yī)學(xué)科學(xué)院醫(yī)學(xué)與健康科技創(chuàng)新工程(2016-I2M-2-002)
【分類號(hào)】：R96
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本文編號(hào)：2256628