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Leflunomide

CAS No. : 75706-12-6

MCE 国际站：Leflunomide

产品活性：Leflunomide 是一种嘧啶合成抑制剂，通过抑制二氢乳清酸脱氢酶 (DHODH) 起作用，具有抗风湿的作用。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Dihydroorotate Dehydrogenase  |  Endogenous Metabolite  |  Bacterial

In Vitro: Leflunomide is actually a prodrug that has been shown to inhibit proliferation of mononuclear and T-cells. Leflunomide is an inhibitor of several protein tyrosine kinases, with IC₅₀ values between 30 mM and 100 mM in vitro cellular and enzymatic assays.
Leflunomide is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. Leflunomide is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. Leflunomide also inhibits Ca²⁺ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. Leflunomide also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. Leflunomide also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2.
Leflunomide is an immunomodulatory drug that may exert its effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which plays a key role in the de novo synthesis of the pyrimidine ribonucleotide uridine monophosphate (rUMP). Leflunomide prevents the expansion of activated and autoimmune lymphocytes by interfering with the cell cycle progression due to inadequate production of rUMP and utilizing mechanisms involving p53.

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