Integrins are cell surface receptors involved in the integration between extracellular and intracellular signals in many biological processes, including cytoskeletal organization and cell adhesion, migration, proliferation, differentiation, and survival. During an immune response,
integrins mediate cell adhesion to the extracellular matrix, and cell-cell interactions (e.g., T cell activation), which are central to the pathology of many inflammatory diseases, including dry eye disease (DED)[2]. Lifitegrast is a novel small molecule integrin antagonist that blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), thus interrupting the T cell-mediated inflammatory cycle[2]. Lifitegrast demonstrated concentration-dependent inhibition of Jurkat cell attachment with an IC50 value of 2.98 nM, suggesting it to be a potent antagonist of LFA-1/ICAM-1–mediated T-cell binding. Lifitegrast also demonstrated potent concentration-dependent inhibition of superantigen induced inflammatory cytokine release from human PBMCs, particularly the Th1 and Th2 T-cell cytokines, IFN-γ and IL-4, respectively. In normal healthy beagles, lifitegrast was well tolerated at concentrations as high as 10% with no apparent adverse effects on the cornea surface or overall ocular health[3].
Lifitegrast/立他司特 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nicotiana benthamiana
TMV-GFP infection model
Foliar spray
0.1 μM BL
Single treatment, observed at 3, 5, and 7 days post inoculation
To investigate the role of BRs in plant resistance to TMV, results showed that BL treatment enhanced plant resistance to virus.
Sci Rep. 2016 Feb 3;6:20579.
Barley
Salt stress model
Foliar spray
10 µM, 50 µM, 100 µM
Single treatment, continued until the 5th leaf growth stage
To study the effect of bikinin on barley growth under salt stress, results showed that bikinin treatment improved growth parameters of barley under salt stress.
Int J Mol Sci. 2022 Oct 1;23(19):11644
Arabidopsis
Bin2-3 bil1 bil2 and bin2-1 mutants
Grown on medium
10 μM ABA
10 days
To investigate the positive regulatory role of BIN2 and its homologs in ABA signaling
Proc Natl Acad Sci U S A. 2014 Jul 1;111(26):9651-6
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