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Literature summary for 3.4.21.75 extracted from

  • Dahms, S.O.; Hardes, K.; Steinmetzer, T.; Than, M.E.
    X-ray structures of the proprotein convertase furin bound with substrate analogue inhibitors reveal substrate specificity determinants beyond the S4 pocket (2018), Biochemistry, 57, 925-934 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
transient expression of homogeneously glycosylated His-tagged furin in HEK-293S cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
purified recombinant His-tagged enzyme in complexes with three peptide-derived inhibitors, vapor diffusion method, mixing of 9 mg/ml protein in 10 mM HEPES, pH 7.5, 100 mM NaCl, and 2 mM CaCl2, with an equal volume of crystallization solution containing 100 mM MES, 200 mM K/NaH2PO4, pH 5.5-6.0, 3-4 M NaCl, and 3% dimethyl sulfoxide, and equilibration against reservoir solution containing 3-4 M NaCl, 20°C, crystals are soaked for about 16 h in a soaking solution conatining 3.16 M NaCl, 100 mM MES/NaOH, pH 5.5, 200 mM Na/KH2PO4, and 1 mM CaCl2 and supplemented with 2 mM Arg-Arg-Arg-Val-Arg-4-aminomethyl-benzamidine, or 1 mM phenylacetyl-Cit-Val-Arg-4-aminomethyl-benzamidine, or 1 mM 4-aminomethyl-phenylacetyl-Arg-Tle-Arg-4-aminomethyl-benzamidine, X-ray diffraction structure determination and analysis at 1.9-2.0 A resolution Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-aminomethyl-phenylacetyl-Arg-Tle-Arg-4-aminomethyl-benzamidine
-
Homo sapiens
acetyl-Val-Arg-4-aminomethyl-benzamidine
-
Homo sapiens
Arg-Arg-Arg-Val-Arg-4-aminomethyl-benzamidine
-
Homo sapiens
additional information analysis of the interactions of P4-P6 of furin with substrate-like peptide inhibitors using X-ray crystallography, substrate specificity is mediated at these binding sites, docking study, detailed overview Homo sapiens
phenylacetyl-Arg-Val-Arg-4-aminomethyl-benzamidine
-
Homo sapiens
phenylacetyl-Cit-Arg-Val-Arg-4-aminomethyl-benzamidine
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09958
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant glycosylated His-tagged furin from HEK-293S cells by nickel affinity and inhibitor affinity chromatography, followed by gel filtration Homo sapiens

Synonyms

Synonyms Comment Organism
Proprotein convertase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000000000224
-
4-aminomethyl-phenylacetyl-Arg-Tle-Arg-4-aminomethyl-benzamidine pH and temperature not specified in the publication Homo sapiens
0.0000000000337
-
Arg-Arg-Arg-Val-Arg-4-aminomethyl-benzamidine pH and temperature not specified in the publication Homo sapiens
0.00000081
-
phenylacetyl-Arg-Val-Arg-4-aminomethyl-benzamidine pH and temperature not specified in the publication Homo sapiens
0.000238
-
phenylacetyl-Cit-Arg-Val-Arg-4-aminomethyl-benzamidine pH and temperature not specified in the publication Homo sapiens
0.0024
-
acetyl-Val-Arg-4-aminomethyl-benzamidine pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
additional information X-ray structures of the proprotein convertase furin bound with substrate analogue inhibitors reveal substrate specificity determinants beyond the S4 pocket, overview. Substrate specificity is mediated at the P4-P6 binding sites of furin Homo sapiens
physiological function proprotein convertase furin is a highly specific serine protease modifying and thereby activating proteins in the secretory pathway by proteolytic cleavage. Its substrates are involved in many diseases, including cancer and infections caused by bacteria and viruses Homo sapiens