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Literature summary for 3.4.21.109 extracted from

  • Sisay, M.T.; Steinmetzer, T.; Stirnberg, M.; Maurer, E.; Hammami, M.; Bajorath, J.; Guetschow, M.
    Identification of the first low-molecular-weight inhibitors of matriptase-2 (2010), J. Med. Chem., 53, 5523-5535.
    View publication on PubMed
Search for more literature for 3.4.21.109

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-MT2 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Aprotinin
-
 Homo sapiens
benzylsulfonyl-D-arginyl-proline-(2-aminomethyl-5-chlorobenzyl)-amide bis(trifluoroacetate)
-
 Homo sapiens
benzylsulfonyl-D-arginyl-proline-(4-amidinobenzyl)amide bis-(trifluoroacetate)
-
 Homo sapiens
benzylsulfonyl-D-cyclohexylalanyl-proline-(2-aminomethyl-5-chlorobenzyl)amide
-
 Homo sapiens
benzylsulfonyl-D-cyclohexylalanyl-proline-(4-amidinobenzyl)-amide
-
 Homo sapiens
leupeptin
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.159
-
 butyloxycarbonyl-L-Gln-L-Ala-L-Arg-4-nitroanilide purified matriptase-2, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.21
-
 butyloxycarbonyl-L-Gln-L-Ala-L-Arg-4-nitroanilide matriptase-2 in conditioned medium of HEK-MT2 cells, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.381
-
 butyloxycarbonyl-L-Gln-L-Ala-L-Arg-4-nitroanilide recombinant human matriptase, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
30000
-
 x * 30000, catalytic domain of matriptase-2, SDS-PAGE Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
butyloxycarbonyl-L-Gln-L-Ala-L-Arg-4-nitroanilide + H2O Homo sapiens
-
 butyloxycarbonyl-L-Gln-L-Ala-L-Arg + 4-nitroaniline
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyloxycarbonyl-L-Gln-L-Ala-L-Arg-4-nitroanilide + H2O
-
 Homo sapiens butyloxycarbonyl-L-Gln-L-Ala-L-Arg + 4-nitroaniline
-
 ?

Subunits

Subunits Comment Organism
? x * 30000, catalytic domain of matriptase-2, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
matriptase-2
-
 Homo sapiens
TMPRSS6
-
 Homo sapiens
transmembrane serine protease 6
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000005
-
 Aprotinin matriptase-2 in conditioned medium of HEK-MT2 cells, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.0000098
-
 Aprotinin recombinant human matriptase, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.000013
-
 Aprotinin purified matriptase-2, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.000055
-
 benzylsulfonyl-D-arginyl-proline-(4-amidinobenzyl)amide bis-(trifluoroacetate) recombinant human matriptase, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.00017
-
 benzylsulfonyl-D-arginyl-proline-(4-amidinobenzyl)amide bis-(trifluoroacetate) purified matriptase-2, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.00019
-
 benzylsulfonyl-D-arginyl-proline-(4-amidinobenzyl)amide bis-(trifluoroacetate) matriptase-2 in conditioned medium of HEK-MT2 cells, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.00022
-
 benzylsulfonyl-D-arginyl-proline-(2-aminomethyl-5-chlorobenzyl)-amide bis(trifluoroacetate) recombinant human matriptase, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.00029
-
 benzylsulfonyl-D-cyclohexylalanyl-proline-(4-amidinobenzyl)-amide matriptase-2 in conditioned medium of HEK-MT2 cells, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.00046
-
 benzylsulfonyl-D-cyclohexylalanyl-proline-(4-amidinobenzyl)-amide purified enzyme, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.00077
-
 benzylsulfonyl-D-cyclohexylalanyl-proline-(4-amidinobenzyl)-amide recombinant human matriptase, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.0019
-
 leupeptin recombinant human matriptase, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.0021
-
 benzylsulfonyl-D-cyclohexylalanyl-proline-(2-aminomethyl-5-chlorobenzyl)amide recombinant human matriptase, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.0024
-
 leupeptin matriptase-2 in conditioned medium of HEK-MT2 cells, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.0041
-
 leupeptin purified matriptase-2, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.01
-
 benzylsulfonyl-D-arginyl-proline-(2-aminomethyl-5-chlorobenzyl)-amide bis(trifluoroacetate) Ki above 0.01 mM, matriptase-2 in conditioned medium of HEK-MT2 cells, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.01
-
 benzylsulfonyl-D-cyclohexylalanyl-proline-(2-aminomethyl-5-chlorobenzyl)amide Ki above 0.01 mM, matriptase-2 in conditioned medium of HEK-MT2 cells, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.01
-
 benzylsulfonyl-D-arginyl-proline-(2-aminomethyl-5-chlorobenzyl)-amide bis(trifluoroacetate) Ki above 0.01 mM, purified matriptase-2, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens
0.01
-
 benzylsulfonyl-D-cyclohexylalanyl-proline-(2-aminomethyl-5-chlorobenzyl)amide Ki above 0.01 mM, purified matriptase-2, in Tris saline buffer (50 mM Tris, 150 mM NaCl, pH 8.0) at 37°C Homo sapiens