| Residential College | false |
| Status | 已發表Published |
| Small molecule inhibitors of RORγt for Th17 regulation in inflammatory and autoimmune diseases | |
| Zeng, Jiuping1,2; Li, Mingxing1,2,3; Zhao, Qianyun1,2; Chen, Meijuan1; Zhao, Long4; Wei, Shulin1,2; Yang, Huan1,2; Zhao, Yueshui1,2,3; Wang, Anqi5; Shen, Jing1,2,3; Du, Fukuan1,2,3; Chen, Yu1,2,3; Deng, Shuai1,2,3; Wang, Fang1,2; Zhang, Zhuo1,2; Li, Zhi4; Wang, Tiangang4; Wang, Shengpeng6; Xiao, Zhangang1,7; Wu, Xu1,6 | |
| 2023-06-01 | |
| Source Publication | Journal of Pharmaceutical Analysis
 |
| ISSN | 2095-1779 |
| Volume | 13Issue:6Pages:545-562 |
| Abstract | As a ligand-dependent transcription factor, retinoid-associated orphan receptor γt (RORγt) that controls T helper (Th) 17 cell differentiation and interleukin (IL)-17 expression plays a critical role in the progression of several inflammatory and autoimmune conditions. An emerging novel approach to the therapy of these diseases thus involves controlling the transcriptional capacity of RORγt to decrease Th17 cell development and IL-17 production. Several RORγt inhibitors including both antagonists and inverse agonists have been discovered to regulate the transcriptional activity of RORγt by binding to orthosteric- or allosteric-binding sites in the ligand-binding domain. Some of small-molecule inhibitors have entered clinical evaluations. Therefore, in current review, the role of RORγt in Th17 regulation and Th17-related inflammatory and autoimmune diseases was highlighted. Notably, the recently developed RORγt inhibitors were summarized, with an emphasis on their optimization from lead compounds, efficacy, toxicity, mechanisms of action, and clinical trials. The limitations of current development in this area were also discussed to facilitate future research. |
| Keyword | Autoimmune disease Inflammatory disease RORγt Small-molecule inhibitor T helper 17 |
| DOI | 10.1016/j.jpha.2023.05.009 |
| URL | View the original |
| Language | 英語English |
| Scopus ID | 2-s2.0-85163377803 |
| Fulltext Access | |
| Citation statistics | |
| Document Type | Journal article |
| Collection | University of Macau |
| Affiliation | 1.Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, 646000, China 2.Cell Therapy & Cell Drugs of Luzhou Key Laboratory, Luzhou, Sichuan, 646000, China 3.South Sichuan Institute of Translational Medicine, Luzhou, Sichuan, 646000, China 4.Department of Spleen and Stomach Diseases, The Affiliated Traditional Chinese Medicine Hospital of Southwest Medical University, Luzhou, Sichuan, 646000, China 5.School of Medicine, Chengdu University, Chengdu, 610106, China 6.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, 999078, China 7.Department of Oncology, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, 646000, China |
| Recommended Citation GB/T 7714 | Zeng, Jiuping,Li, Mingxing,Zhao, Qianyun,et al. Small molecule inhibitors of RORγt for Th17 regulation in inflammatory and autoimmune diseases[J]. Journal of Pharmaceutical Analysis, 2023, 13(6), 545-562. |
| APA | Zeng, Jiuping., Li, Mingxing., Zhao, Qianyun., Chen, Meijuan., Zhao, Long., Wei, Shulin., Yang, Huan., Zhao, Yueshui., Wang, Anqi., Shen, Jing., Du, Fukuan., Chen, Yu., Deng, Shuai., Wang, Fang., Zhang, Zhuo., Li, Zhi., Wang, Tiangang., Wang, Shengpeng., Xiao, Zhangang., & Wu, Xu (2023). Small molecule inhibitors of RORγt for Th17 regulation in inflammatory and autoimmune diseases. Journal of Pharmaceutical Analysis, 13(6), 545-562. |
| MLA | Zeng, Jiuping,et al."Small molecule inhibitors of RORγt for Th17 regulation in inflammatory and autoimmune diseases".Journal of Pharmaceutical Analysis 13.6(2023):545-562. |
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