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Literature summary for 3.4.21.75 extracted from

  • Shiryaev, S.A.; Remacle, A.G.; Ratnikov, B.I.; Nelson, N.A.; Savinov, A.Y.; Wei, G.; Bottini, M.; Rega, M.F.; Parent, A.; Desjardins, R.; Fugere, M.; Day, R.; Sabet, M.; Pellecchia, M.; Liddington, R.C.; Smith, J.W.; Mustelin, T.; Guiney, D.G.; Lebl, M.; Strongin, A.Y.
    Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens (2007), J. Biol. Chem., 282, 20847-20853.
    View publication on PubMed

Application

Application Comment Organism
medicine inhibiting furin-like proprotein convertases protects the host from the distinct furin-dependent infections and lay a foundation for novel, host cell-focused therapies against acute diseases Mus musculus
medicine inhibiting furin-like proprotein convertases protects the host from the distinct furin-dependent infections and lay a foundation for novel, host cell-focused therapies against acute diseases Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
recombinant furin prepared in the S2 Drosophila expression system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
decanoyl-Arg-Val-Lys-Arg-chloromethylketone
-
Homo sapiens
TPQRARRRKKRF
-
Homo sapiens
TPQRARRRKKRT
-
Homo sapiens
TPQRARRRKKRW
-
Homo sapiens
TPQRARRRKKRY
-
Homo sapiens
TPRARRRKKRG
-
Homo sapiens
TPRARRRKKRI
-
Homo sapiens
TPRARRRKKRT
-
Homo sapiens
TPRARRRKKRT
-
Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
C57/BL6 mice
-
Mus musculus C57BL/6
-
C57/BL6 mice
-

Purification (Commentary)

Purification (Comment) Organism
to homogeneity Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
hemagglutinin + H2O
-
Homo sapiens ?
-
?
PA83 + H2O
-
Homo sapiens PA63 + PA20
-
?
Pseudomonas exotoxin A + H2O
-
Mus musculus ?
-
?
Pseudomonas exotoxin A + H2O
-
Homo sapiens ?
-
?
Pseudomonas exotoxin A + H2O
-
Mus musculus C57BL/6 ?
-
?
pyroglutamic acid-Arg-Thr-Lys-Arg-methylcoumaryl-7-amide + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Proprotein convertase
-
Mus musculus
Proprotein convertase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000023
-
TPRARRRKKRT
-
Homo sapiens
0.00003
-
TPRARRRKKRI
-
Homo sapiens
0.000033
-
TPQRARRRKKRT
-
Homo sapiens
0.000034
-
TPQRARRRKKRW
-
Homo sapiens
0.000038
-
TPQRARRRKKRF
-
Homo sapiens
0.000047
-
TPQRARRRKKRY
-
Homo sapiens
0.000057
-
TPRARRRKKRG
-
Homo sapiens