创新链/学科链/研发链/产业链

新药研发前沿动态 / 医药领域趋势进展

吴军, 王亚洲, 杨圣伟, 李志裕. 组蛋白乙酰转移酶p300/CBP抑制剂的研究进展[J]. 药学进展, 2019, 43(2): 118-126.
引用本文: 吴军, 王亚洲, 杨圣伟, 李志裕. 组蛋白乙酰转移酶p300/CBP抑制剂的研究进展[J]. 药学进展, 2019, 43(2): 118-126.
WU Jun, WANG Yazhou, YANG Shengwei, LI Zhiyu. Recent Advances in Inhibitors of Histone Acetyltransferase p300/CBP[J]. Progress in Pharmaceutical Sciences, 2019, 43(2): 118-126.
Citation: WU Jun, WANG Yazhou, YANG Shengwei, LI Zhiyu. Recent Advances in Inhibitors of Histone Acetyltransferase p300/CBP[J]. Progress in Pharmaceutical Sciences, 2019, 43(2): 118-126.

组蛋白乙酰转移酶p300/CBP抑制剂的研究进展

Recent Advances in Inhibitors of Histone Acetyltransferase p300/CBP

  • 摘要: 由高度同源的腺病毒E1A相关的300 kDa蛋白(p300)和环磷酸腺苷反应元件结合蛋白(CREB)的结合蛋白(CBP)组成的p300/CBP家族是组蛋白乙酰转移酶(HAT)家族主要成员之一。p300/CBP参与细胞周期进展和细胞的生长、分化和发展,是一类非常重要的辅激活因子,可以调节多种关键转录调节因子的功能。p300/CBP与多种肿瘤疾病密切相关,是一个极具应用前景的肿瘤治疗靶标。综述p300/CBP抑制剂的研究进展,旨在为开发新型选择性p300/CBP抑制剂提供参考。

     

    Abstract: The p300/CBP family consisting of the highly homologous adenovirus E1A-associated 300 kDa protein (p300) and CREB (cAMP responsive element binding protein) binding protein (CBP) is one of the major members of the histone acetyltransferases families (HAT). Acting as a very important coactivator that can regulate the functions of key transcription regulatory factors, p300/CBP is involved in cell cycle progression as well as cell growth, differentiation and development. Since p300/CBP is also closely related to a variety of tumors, it emerges as a promising target for tumor therapy. This paper reviewed the research progress of p300/CBP inhibitors in order to provide reference for the development of novel selective p300/CBP inhibitors.

     

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