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Literature summary for 3.4.21.75 extracted from

  • Hardes, K.; Ivanova, T.; Thaa, B.; McInerney, G.M.; Klokk, T.I.; Sandvig, K.; Kuenzel, S.; Lindberg, I.; Steinmetzer, T.
    Elongated and shortened peptidomimetic inhibitors of the proprotein convertase furin (2017), ChemMedChem, 12, 613-620 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.75

Inhibitors

Inhibitors Comment Organism Structure
3-guanidinomethylphenylacetyl-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
D-Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
D-Arg-Arg-Tle-Arg 4-amidinobenzylamide
-
 Homo sapiens
D-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
D-Arg-D-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
D-Arg-D-Arg-D-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
D-Arg-D-Arg-D-Arg-D-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
additional information inhibitor constructuion, synthesis, and structure-function analysis, overview. Evaluation of inhibition of alphavirus propagation and inhibition of diphtheria toxin action Homo sapiens
N2(carbamidoyl)Arg-Ala-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2(carbamidoyl)Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-(3-aminomethyl-phenylacetyl)-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-(5-(guanidino)valeroyl)-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-(5-aminopentanoyl)-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-(5-guanidinopentanoly)-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-acetyl-D-Leu-Leu-Leu-Leu-Arg-Val-Lys 4-amidinobenzylamide
-
 Homo sapiens
N2-acetyl-Leu-Leu-Leu-Leu-Arg-Tle-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-acetyl-Leu-Leu-Leu-Leu-Arg-Tle-Lys 4-amidinobenzylamide
-
 Homo sapiens
N2-acetyl-Leu-Leu-Leu-Leu-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-acetyl-Leu-Leu-Leu-Leu-Arg-Val-Lys 4-amidinobenzylamide
-
 Homo sapiens
N2-phenylacetyl-Ala-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-phenylacetyl-Arg-Ala-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-phenylacetyl-Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-phenylacetyl-Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
N2-phenylacetyl-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens
Nalpha(carbamidoyl)Arg-Arg-Val-Arg 4-amidinobenzylamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09958
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
phenylacetyl-Arg-Val-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens phenylacetyl-Arg-Val-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
Proprotein convertase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information Ki values of the inhibitors with inhibition constants above 0.1 nM are determined by fitting of the data to the equation for classical reversible competitive inhibition Homo sapiens
0.0000000062
-
 D-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000119
-
 Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000138
-
 Nalpha(carbamidoyl)Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000283
-
 N2-phenylacetyl-Arg-Ala-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000337
-
 N2-phenylacetyl-Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000378
-
 D-Arg-D-Arg-D-Arg-D-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000459
-
 N2-(5-(guanidino)valeroyl)-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000491
-
 N2-phenylacetyl-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.000000051
-
 N2-phenylacetyl-Ala-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000563
-
 N2-phenylacetyl-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000754
-
 Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000786
-
 N2-acetyl-D-Leu-Leu-Leu-Leu-Arg-Val-Lys 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000000943
-
 D-Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.000000108
-
 D-Arg-D-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.00000011
-
 D-Arg-D-Arg-D-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.000000164
-
 N2-acetyl-Leu-Leu-Leu-Leu-Arg-Val-Lys 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.000000193
-
 N2(carbamidoyl)Arg-Ala-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.000000449
-
 N2(carbamidoyl)Arg-Arg-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.000000491
-
 D-Arg-Arg-Tle-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.00000126
-
 N2-(5-aminopentanoyl)-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000025
-
 3-guanidinomethylphenylacetyl-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000267
-
 N2-(5-guanidinopentanoly)-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000378
-
 N2-acetyl-Leu-Leu-Leu-Leu-Arg-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000385
-
 N2-(5-aminopentanoyl)-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0000482
-
 N2-acetyl-Leu-Leu-Leu-Leu-Arg-Tle-Lys 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.000164
-
 N2-acetyl-Leu-Leu-Leu-Leu-Arg-Tle-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens
0.0002693
-
 N2-(3-aminomethyl-phenylacetyl)-Val-Arg 4-amidinobenzylamide pH 7.0, 22°C Homo sapiens