生物活性 | |||
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描述 | The β2 integrin CD11b/CD18 (also known as Mac-1, aMb2, and CR3),expressed primarily in the cells of the innate immune system,is a key adhesion receptor that mediates leukocyte migration and immune functions. ICAM-1 (CD54),a member of the immunoglobulin family,is expressed on the surface of vascular endothelial cells and mediates migration and tissue recruitment of leukocytes from circulation. Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1. Daily LA1 intraperitoneal treatment at 2.5 mg/kg reduced interstitial leukocyte infiltration in the kidney allograft, reduced neointimal hyperplasia and glomerular damage, and prolonged graft survival from 48.5% (CsA only) to 100% (CsA and LA1) on day 60[3]. LA1 pre-treatment at 7.5 mM reduced secretion of IFN–γ, TNF and MIP-1β by monokine-stimulated Natural Killer (NK) cells which was associated with a decrease in pSTAT5 following IL-12+IL-15 stimulation (P<0.02) and increased IL-10 secretion following IL-12+IL-18 stimulation (P<0.001). Also, LA1 pre-treatment reduced secretion of IL-1β, IL-6 and TNF by Toll-like receptor (TLR) 2 and TLR7/8–stimulated monocytes[4]. | ||
作用机制 | Leukadherin-1 enhances binding of CD11b/CD18 to ICAM-1 via the formation of long membrane tethers. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.37mL 0.47mL 0.24mL |
11.86mL 2.37mL 1.19mL |
23.73mL 4.75mL 2.37mL |
参考文献 |
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