Literature summary for 3.4.21.73 extracted from

Jiang, L.; Zhao, B.; Xu, P.; Soerensen, H.P.; Jensen, J.K.; Christensen, A.; Hosseini, M.; Nielsen, N.C.; Jensen, K.J.; Andreasen, P.A.; Huang, M.
Distinctive binding modes and inhibitory mechanisms of two peptidic inhibitors of urokinase-type plasminogen activator with isomeric P1 residues (2015), Int. J. Biochem. Cell Biol., 62, 88-92.

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Cloned(Commentary)

Cloned (Comment)	Organism
recombinant expression of mutant enzyme	Homo sapiens
recombinant expression of wild-type enzyme	Mus musculus

Crystallization (Commentary)

Crystallization (Comment)	Organism
purified recombinant enzyme mutant H99Y in complex with mupain-1 inhibitor variants, sitting drop vapour diffusion method, equilibrating of protein against a reservoir solution containing 2.0 M ammonium sulfate, 50 mM sodium citrate, pH 4.6, and 5% PEG 400, room temperature, about 3 days, soaking of crystals in 40% PEG 4000, 100 mM Tris-HCl, pH 7.4 containing 1 mM mupain ligand variant, X-ray diffraction structure determination and analysis at 1.6 A resolution	Homo sapiens

Crystallization (Comment)

Organism

purified recombinant enzyme mutant H99Y in complex with mupain-1 inhibitor variants, sitting drop vapour diffusion method, equilibrating of protein against a reservoir solution containing 2.0 M ammonium sulfate, 50 mM sodium citrate, pH 4.6, and 5% PEG 400, room temperature, about 3 days, soaking of crystals in 40% PEG 4000, 100 mM Tris-HCl, pH 7.4 containing 1 mM mupain ligand variant, X-ray diffraction structure determination and analysis at 1.6 A resolution

Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
H99Y	site-directed mutagenesis, structure analysis with bound inhibitors	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
3-(1-carbamimidoylpiperidin-3-yl)-L-alanine	-	Homo sapiens
3-(1-carbamimidoylpiperidin-3-yl)-L-alanine	-	Mus musculus
3-(1-carbamimidoylpiperidin-4-yl)-L-alanine	-	Homo sapiens
3-(1-carbamimidoylpiperidin-4-yl)-L-alanine	-	Mus musculus
mupain-1	i.e. CPAYSRYLDC	Homo sapiens
mupain-1	i.e. CPAYSRYLDC	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Mus musculus	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
recombinant mutant enzyme by dialysis and ultrafiltration	Homo sapiens
recombinant wild-type enzyme by dialysis and ultrafiltration	Mus musculus

Synonyms

Synonyms	Comment	Organism
uPA	-	Mus musculus
uPA	-	Homo sapiens
Urokinase-type plasminogen activator	-	Mus musculus
Urokinase-type plasminogen activator	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Mus musculus
37	-	assay at	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.4	-	assay at	Mus musculus
7.4	-	assay at	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
additional information	-	additional information	inhibition kinetics of mupain variants, overview	Mus musculus
additional information	-	additional information	inhibition kinetics of mupain variants, overview	Homo sapiens
0.00248	-	3-(1-carbamimidoylpiperidin-4-yl)-L-alanine	pH 7.4, 37°C, enzyme mutant H99Y	Homo sapiens
0.0065	-	3-(1-carbamimidoylpiperidin-3-yl)-L-alanine	pH 7.4, 37°C, wild-type enzyme	Mus musculus
0.045	-	3-(1-carbamimidoylpiperidin-4-yl)-L-alanine	pH 7.4, 37°C, wild-type enzyme	Mus musculus
0.219	-	3-(1-carbamimidoylpiperidin-3-yl)-L-alanine	pH 7.4, 37°C, enzyme mutant H99Y	Homo sapiens

General Information

General Information	Comment	Organism
additional information	the enzyme's catalytic domain comprises residues 159-411	Mus musculus
additional information	the enzyme's catalytic domain comprises residues 159-411	Homo sapiens