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Literature summary for 1.3.5.2 extracted from

  • Deguchi, M.; Kishino, J.; Hattori, M.; Furue, Y.; Yamamoto, M.; Mochizuki, I.; Iguchi, M.; Hirano, Y.; Hojou, K.; Nagira, M.; Nishitani, Y.; Okazaki, K.; Yasui, K.; Arimura, A.
    Suppression of immunoglobulin production by a novel dihydroorotate dehydrogenase inhibitor, S-2678 (2008), Eur. J. Pharmacol., 601, 163-170.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
A77 1726 active metabolite of the anti-rheumatic drug leflunomide Homo sapiens
A77 1726 active metabolite of the anti-rheumatic drug leflunomide Mus musculus
[2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine i.e. S-2678, suppresses immunoglobulin production in human peripheral blood mononuclear cells in vitro, with little or no inhibition of cell proliferation Homo sapiens
[2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine i.e. S-2678, suppresses immunoglobulin production in mouse B cells in vitro, with little or no inhibition of cell proliferation, probably through inhibition of class switch recombination in the immunoglobulin heavy chain loci in B cells. In vivo antibody production induced by systemic immunization with ovalbumin is dramatically suppressed by oral administration of S-2678, without any toxicological signs. S-2678 does not affect T-cell activation in vitro, and cytokine production induced by intravenous anti-CD3 antibody in mice. S-2678 does not affect host defense in a mouse model of Candida infection, whereas leflunomide severely impaires it Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Mus musculus
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IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
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 IC50 value 150 ng per ml Mus musculus A77 1726
additional information
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 IC50 value 23 ng per ml Homo sapiens [2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine
additional information
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 IC50 value 32 ng per ml Mus musculus [2-fluoro-2',5'-dimethyl-4'-[6-(3-methyl-2-butenyloxy)pyridin-3-yl]biphenyl-4-yl]-(3-methyl-2-butenyl)amine
additional information
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 IC50 value 440 ng per ml Homo sapiens A77 1726