Cloned (Comment) | Organism |
---|---|
transient expression of homogeneously glycosylated His-tagged furin in HEK-293S cells | Homo sapiens |
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 | 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 | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | required | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P09958 | - |
- |
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 | Comment | Organism |
---|---|---|
Proprotein convertase | - |
Homo sapiens |
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 | 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 |