Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues
文献类型：期刊论文
| 作者 | Du, Guoxin1,2; Du, Weiwei1,2; An, Yuanlong1,2; Wang, Minnan3; Hao, Feifei2; Tong, Xiaochu4; Gong, Qi2,3; He, Xiangdong1,2,3; Jiang, Hualiang4 ; He, Wei1
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| 刊名 | MEDICINAL CHEMISTRY RESEARCH
 |
| 出版日期 | 2022-02-17 |
| 页码 | 25 |
| ISSN号 | 1054-2523 |
| 关键词 | Lifitegrast Analogues LFA-1/ICAM-1 antagoinst Dry eye Corneal epithelial in jury |
| DOI | 10.1007/s00044-022-02851-9 |
| 通讯作者 | Zheng, Mingyue(myzheng@simm.ac.cn) ; Zhang, Donglei(zhangdonglei@huh.edu.cn) |
| 英文摘要 | The interaction between Lymphocyte function-associated antigen 1 (LFA-1) and intercellular-adhesion molecule-1 (ICAM-1) plays important roles in the cell-mediated immune response and inflammation associated with dry eye disease. LFA-1/ICAM-1 antagonists can be used for the treatment of dry eye disease, such as Lifitegrast which has been approved by the FDA in 2016 as a new drug for the treatment of dry eye disease. In this study, we designed and synthesized some new structure compounds that are analogues to Lifitegrast, and their biological activities were evaluated by in vitro cell-based assay and also by in vivo mouse dry eye model. Our results demonstrated that one of these analogues of Lifitegrast (compound 1b) showed good LFA-1/ICAM-1 antagonist activity in in vitro assay; meanwhile, it also significantly reduced ocular surface epithelial cells damage, increased goblet cell density in dry eye mouse and highly improved the symptoms of dry eye mouse. [GRAPHICS] . |
| WOS关键词 | DRY EYE DISEASE ; OPHTHALMIC SOLUTION ; DISCOVERY ; POTENT ; CONJUNCTIVA ; DERIVATIVES ; INHIBITORS ; ADHESION ; LIGAND ; ICAM-1 |
| 资助项目 | Technology Program of Liaoning[2019JH2/10300011] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | SPRINGER BIRKHAUSER |
| WOS记录号 | WOS:000756249700001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/300442]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zheng, Mingyue; Zhang, Donglei |
| 作者单位 | 1.He Univ, Sch Pharm, Shenyang 110163, Peoples R China 2.Shenyang Ind Technol Inst Ophthalmol, Shenyang 110163, Peoples R China 3.Shenyang He Vis Ind Grp Co Ltd, Shenyang 110163, Peoples R China 4.Chinese Acad Sci, Drug Discovery & Design Ctr, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Du, Guoxin,Du, Weiwei,An, Yuanlong,et al. Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues[J]. MEDICINAL CHEMISTRY RESEARCH,2022:25. |
| APA | Du, Guoxin.,Du, Weiwei.,An, Yuanlong.,Wang, Minnan.,Hao, Feifei.,...&Zhang, Donglei.(2022).Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues.MEDICINAL CHEMISTRY RESEARCH,25. |
| MLA | Du, Guoxin,et al."Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues".MEDICINAL CHEMISTRY RESEARCH (2022):25. |
入库方式： OAI收割
来源：上海药物研究所
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