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Literature summary for 3.4.21.7 extracted from

  • Li, Q.; Laumonnier, Y.; Syrovets, T.; Simmet, T.
    Plasmin triggers cytokine induction in human monocyte-derived macrophages (2007), Arterioscler. Thromb. Vasc. Biol., 27, 1383-1389.
    View publication on PubMed
Search for more literature for 3.4.21.7

Application

Application Comment Organism
medicine plasmin generated in atherosclerotic lesion can induce macrophage activation Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
AG490 JAK inhibitor, inhibits JAK1 but does not inhibit TYK2 phosphorylation by plasmin. Impairs plasmin-mediated phosphorylation of ERK1/2, Akt1, and the subsequent phosphorylation of IkappaBalpha, but not that of p38 MAPK. Inhibits plasmin-induced TNF-alpha release by 63% and IL-6 release by 76% Homo sapiens
AKbetaBA inhibits plasmin-induced TNF-alpha release by 70%. Inhibits plasmin-induced activation of NF-kappaB by 66% Homo sapiens
additional information inhibition of ERK1/2 by MEK inhibitor U0126 does not affect plasmin-mediated expression of TNF-alpha Homo sapiens
SB203580 inhibits plasmin-induced TNF-alpha release by 75% and IL-6 release by 79% Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
macrophage plasmin triggers expression and release of proinflammatory cytokines such as TNF-alpha and IL-6 in human monocyte-derived macrophages with a somewhat lower potency than the standard stimulus lipopolysaccharide. Plasmin-induced activation of JAK1, p38, ERK1/2, and NF-kappaB is indispensable for the cytokine expression Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
annexin A2 + H2O stimulation of macrophages with plasmin leads to cleavage of ca. 6% of annexin A2 yielding a proteolytic fragment of ca. 33 kDa Homo sapiens ?
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ERK1/2 triggers activation Homo sapiens ?
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IkappaBalpha plasmin induces phosphorylation of IkappaBalpha, targeting the inhibitor to proteosomal degradation, consequently allowing nuclear translocation of NF-kappaB Homo sapiens ?
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JAK1 triggers tyrosine phosphorylation Homo sapiens ?
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additional information plasmin does not induce phosphorylation of JAK2 or JAK3. Does not activate SAP/JNK. Does not trigger activation and nuclear translocation ofSTAT1, STAT5A, or STAT5B Homo sapiens ?
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p38 MAPK triggers phosphorylation Homo sapiens ?
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p65 triggeres nuclear translocation Homo sapiens ?
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STAT3 phosphorylates on Tyr705 and Ser727. Triggeres activation and nuclear translocation of STAT3 Homo sapiens ?
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TYK2 triggers tyrosine phosphorylation Homo sapiens ?
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