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Literature summary for 3.4.21.75 extracted from

  • Kuester, M.; Becker, G.L.; Hardes, K.; Lindberg, I.; Steinmetzer, T.; Than, M.E.
    Purification of the proprotein convertase furin by affinity chromatography based on PC-specific inhibitors (2011), Biol. Chem., 392, 973-981.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
acetyl-Val-Arg-4-amidinobenzylamide
-
Mus musculus
biotin-(8-(amino)-3,6-dioxa-octanoyl)2-Arg-Pro-Arg-4-amidinobenzylamide
-
Mus musculus
biotin-(8-(amino)-3,6-dioxa-octanoyl)2-Arg-Thr-Arg-4-amidinobenzylamide
-
Mus musculus
biotin-(8-(amino)-3,6-dioxa-octanoyl)3-Arg-Pro-Arg-4-amidinobenzylamide
-
Mus musculus
biotin-8-(amino)-3,6-dioxa-octanoyl-Arg-Pro-Arg-4-amidinobenzylamide
-
Mus musculus
biotin-8-(amino)-3,6-dioxa-octanoyl-Val-Arg-4-amidinobenzylamide
-
Mus musculus
phenylacetyl-Arg-Pro-Arg-4-amidinobenzylamide
-
Mus musculus
phenylacetyl-Arg-Thr-Arg-4-amidinobenzylamide
-
Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
purification protocol combining the heterologous expression of furin from CHO cells with an affinity step that efficiently extracts only active furin from the conditioned medium by using furin-specific inhibitor moieties as bait. The best affinity tag used, biotin-(8-(amino)-3,6-dioxa-octanoyl)2-Arg-Pro-Arg-4-4-amidinobenzylamide coupled to streptavidin-Sepharose beads, is used in a three-step chromatographic protocol and routinely results in a high yield of a homogeneous furin preparation with a specific activity of about 60 units/mg protein Mus musculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Pyr-Arg-Thr-Lys-Arg-4-methylcoumarin 7-amide + H2O
-
Mus musculus Pyr-Arg-Thr-Lys-Arg + 7-amino-4-methylcoumarin
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000006
-
phenylacetyl-Arg-Thr-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus
0.000009
-
biotin-(8-(amino)-3,6-dioxa-octanoyl)2-Arg-Thr-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus
0.0000151
-
biotin-(8-(amino)-3,6-dioxa-octanoyl)3-Arg-Pro-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus
0.0000367
-
phenylacetyl-Arg-Pro-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus
0.0000383
-
biotin-8-(amino)-3,6-dioxa-octanoyl-Arg-Pro-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus
0.0000574
-
biotin-(8-(amino)-3,6-dioxa-octanoyl)2-Arg-Pro-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus
0.00239
-
acetyl-Val-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus
0.0042
-
biotin-8-(amino)-3,6-dioxa-octanoyl-Val-Arg-4-amidinobenzylamide pH 7.0, 37°C Mus musculus