Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists | |
Wu Xishan1; Wang Rui2; Xing Yanli2; Xue Xiaoqian2; Zhang Yan2; Lu Yongzhi2; Song Yu2; Luo Xiaoyu2; Wu Chun2; Zhou Yulai4 | |
刊名 | ACTA PHARMACOLOGICA SINICA
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2016 | |
卷号 | 37期号:11页码:1516 |
关键词 | GAMMA-T ORPHAN RECEPTORS CELL-DIFFERENTIATION LIGAND IDENTIFICATION MODULATORS DERIVATIVES PROTEIN INHIBITORS DOCKING nuclear receptor RORc inverse agonist SAR structure-based optimization autoimmune disease |
ISSN号 | 1671-4083 |
英文摘要 | Aim: Retinoic acid receptor-related orphan nuclear receptors (RORs) are orphan nuclear receptors that show constitutive activity in the absence of ligands. Among 3 subtypes of RORs, RORc is a promising therapeutic target for the treatment of Th17-mediated autoimmune diseases. Here, we report novel RORc inverse agonists discovered through structure-based drug design. |
资助项目 | [National Natural Science Foundation of China] ; ["100 Talents Project" of Chinese Academy of Sciences] ; [Natural Science Foundation of Guangdong Province] ; [Guangzhou Healthcare Collaborative Innovation Programs] ; [Chinese Academy of Sciences Cloud Platform for Stem Cell and Biomedical Research] ; [National Key Basic Research Program of China (973 Program)] ; [Bureau of Science and Information Technology of Guangzhou Municipality] ; [Guangzhou Branch of the Supercomputing Center of Chinese Academy of Sciences] |
语种 | 英语 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/293849] ![]() |
专题 | 中国科学院上海药物研究所 |
作者单位 | 1.中国科学院上海药物研究所 2.中国科学院 3.中国科学院大学 4.吉林大学 |
推荐引用方式 GB/T 7714 | Wu Xishan,Wang Rui,Xing Yanli,et al. Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists[J]. ACTA PHARMACOLOGICA SINICA,2016,37(11):1516. |
APA | Wu Xishan.,Wang Rui.,Xing Yanli.,Xue Xiaoqian.,Zhang Yan.,...&Xu Yong.(2016).Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists.ACTA PHARMACOLOGICA SINICA,37(11),1516. |
MLA | Wu Xishan,et al."Discovery and structural optimization of 4-(4-(benzyloxy) phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists".ACTA PHARMACOLOGICA SINICA 37.11(2016):1516. |
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