Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
Vedolizumab (anti-α4β7-integrin) binds to a subset of human peripheral blood memory CD4+ T lymphocytes including gut-homing interleukin 17 T-helper lymphocytes at the highest level, also binds to eosinophils at high levels, and to naive T-helper lymphocytes, naive and memory cytotoxic T lymphocytes, B lymphocytes, natural killer cells, and basophils at lower levels; Vedolizumab binds to memory CD4+ T and B lymphocytes with subnanomolar potency with EC50 of 0.3-0.4 nM.[1]
[1] Soler D, et al. J Pharmacol Exp Ther. 2009 Sep;330(3):864-75.
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Kinase experiment: |
Vedolizumab inhibition of high-affinity binding of MAdCAM-1 to human peripheral blood memory CD4+ T lymphocytes is tested. Peripheral blood (90 μL) is incubated with a saturating concentration (3 μg/mL) of MAdCAM-1-murine-Fc fusion protein and 4 mM MnCl2 in a final volume of 100 μL for 1 h at room temperature, in the presence or absence of vedolizumab. After washing with assay buffer, the cells are stained with fluorescentlabeled anti-mouse IgG for 15 min at room temperature. After washing again, cells are incubated with mouse serum for 10 min at room temperature, followed by staining with anti-CD4 and anti-CD45RO antibodies for 15 min at room temperature. After washing, red blood cells are lysed with BD FACS lysing solution and analyzed by flow cytometry in a FACSCalibur with CellQuest Pro software[1]. |
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参考文献: [1]. Soler D, et al. The binding specificity and selective antagonism of vedolizumab, an anti-alpha4beta7 integrintherapeutic antibody in development for inflammatory bowel diseases. J Pharmacol Exp Ther. 2009 Sep;330(3):864-75. |
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