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- W4213217190 abstract "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. Graphical abstract." @default.
- W4213217190 created "2022-02-24" @default.
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- W4213217190 date "2022-02-17" @default.
- W4213217190 modified "2023-09-27" @default.
- W4213217190 title "Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues" @default.
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- W4213217190 doi "https://doi.org/10.1007/s00044-022-02851-9" @default.
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