探索用于治疗类风湿性关节炎的基于1,3 - 二氨基嘧啶的布鲁顿酪氨酸激酶共价抑制剂的活性构象。
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.
作者信息
Huang Zhenhua, Zhang Qian, Yan Lianzhong, Zhong Guizhen, Zhang Linqi, Tan Xiaojuan, Wang Yanli
机构信息
KBP Biosciences, C201, No. 750, Shunhua Road, Jinan, Shandong Province 250101, China.
KBP Biosciences, C201, No. 750, Shunhua Road, Jinan, Shandong Province 250101, China.
出版信息
Bioorg Med Chem Lett. 2016 Apr 15;26(8):1954-7. doi: 10.1016/j.bmcl.2016.03.011. Epub 2016 Mar 4.
By applying conformational restrictions, we were able to discover highly potent 1,3-diaminopyrimidine based covalent inhibitors of BTK, such as 8a (IC50=3.76 nM), and providing useful information of its active conformation. We are developing these novel small molecule covalent inhibitors of BTK toward oral agents for Rheumatoid arthritis.
通过应用构象限制，我们能够发现基于1,3 - 二氨基嘧啶的高效BTK共价抑制剂，如8a（IC50 = 3.76 nM），并提供其活性构象的有用信息。我们正在将这些新型的BTK小分子共价抑制剂开发为用于类风湿性关节炎的口服药物。
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