基于多向药理学的BET Bromodomain抑制剂及降解剂研究进展
发布时间：2019-06-12 07:46
【摘要】：溴结构域和末端外结构域(BET)Bromodomain已成为可用于治疗癌症和其他人类疾病的新靶标。目前已发现了几类有效的选择性小分子BET Bromodomain抑制剂,且多种已处于临床开发中。临床前和临床数据已证明BET Bromodomain抑制剂有良好的前景,但也存在耐药性等潜在缺陷。目前人们正在尝试将具有不同作用机制的靶标与BET Bromodomain组合,开发基于多向药理学的BET Bromodomain抑制剂及降解剂。本文综述了激酶/BET小分子抑制剂、组蛋白去乙酰化酶/BET小分子抑制剂及BET蛋白降解剂,为后续针对BET蛋白更深入的研究提供思路。
[Abstract]:Bromine domain and terminal domain (BET) Bromodomain have become new targets for the treatment of cancer and other human diseases. At present, several kinds of effective selective small molecule BET Bromodomain inhibitors have been found, and many of them are in clinical development. Preclinical and clinical data have proved that BET Bromodomain inhibitors have a good prospect, but there are also potential defects such as drug resistance. At present, people are trying to combine targets with BET Bromodomain with different mechanisms to develop BET Bromodomain inhibitors and degradation agents based on multidirectional pharmacology. In this paper, kinase / BET small molecule inhibitor, histone deacetylase / BET small molecule inhibitor and BET protein degradation agent are reviewed, which provides ideas for further research on BET protein.
【作者单位】： 中国药科大学理学院;浙江省医学科学院药物研究所;
【基金】：国家自然科学基金资助项目(81473077) 江苏省高校“青蓝工程”资助项目
【分类号】：R96
本文编号：2497851
[Abstract]:Bromine domain and terminal domain (BET) Bromodomain have become new targets for the treatment of cancer and other human diseases. At present, several kinds of effective selective small molecule BET Bromodomain inhibitors have been found, and many of them are in clinical development. Preclinical and clinical data have proved that BET Bromodomain inhibitors have a good prospect, but there are also potential defects such as drug resistance. At present, people are trying to combine targets with BET Bromodomain with different mechanisms to develop BET Bromodomain inhibitors and degradation agents based on multidirectional pharmacology. In this paper, kinase / BET small molecule inhibitor, histone deacetylase / BET small molecule inhibitor and BET protein degradation agent are reviewed, which provides ideas for further research on BET protein.
【作者单位】： 中国药科大学理学院;浙江省医学科学院药物研究所;
【基金】：国家自然科学基金资助项目(81473077) 江苏省高校“青蓝工程”资助项目
【分类号】：R96
【相似文献】
相关会议论文 前1条
1 佟立纯;谷音;武贺;闫峰;杨立新;;农残降解剂降解除草剂——阿特拉津效果好[A];辽宁省昆虫学会2006年年会论文集[C];2006年
相关重要报纸文章 前3条
1 北京绿色太阳零农残研究院 战井春;战氏生物农残降解剂 在南方植物上的应用[N];消费日报;2007年
2 威海市供销合作社 祝桂强;消除农残改善农产品品质[N];消费日报;2007年
3 本报记者 李文华邋实习生 桑大伟;农药降解剂问世[N];市场报;2008年
相关硕士学位论文 前1条
1 宋亮;农药降解剂对不同农药的降解效果及在不同作物上的应用研究[D];浙江大学;2013年
，本文编号：2497851
本文链接：https://www.wllwen.com/yixuelunwen/yiyaoxuelunwen/2497851.html
最近更新
教材专著
