Literature summary for 3.4.21.73 extracted from

Zeslawska, E.; Jacob, U.; Schweinitz, A.; Coombs, G.; Bode, W.; Madison, E.
Crystals of urokinase type plasminogen activator complexes reveal the binding mode of peptidomimetic inhibitors (2003), J. Mol. Biol., 328, 109-118.

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Cloned(Commentary)

Cloned (Comment)	Organism
mutant C122S expressed in Escherichia coli inclusion bodies, B-chain uPA expressed in S. pastoris	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
beta-c-uPA in complex with inhibitor UPA-I1, space group P2(1)2(1)2(1), cell constants a = 53.2 A, b = 54.7 A, c = 82.4 A, beta-c-uPA in complex with inhibitor UPA-I3, space group P2(1)2(1)2(1), cell constants a = 52.9 A, b = 54.7 A, c = 81.4 A, beta-c-uPA in complex with inhibitor UPA-I2, space group P2(1)2(1)2(1), cell constants a = 53.0 A, b = 54.4 A, c = 82.2 A, beta-c-uPA in complex with inhibitor UPA-I5, space group P2(1)2(1)2(1), cell constants a = 53.0 A, b = 54.9 A, c = 82.3 A, beta-c-uPA in complex with inhibitor UPA-I6, space group P2(1)2(1)2(1), cell constants a = 53.5 A, b = 54.8 A, c = 82.4 A, complex by soaking, Ybeta-c-uPA in complex with inhibitor UPA-I6, space group P4(3)2(1)2, cell constants a = 76.7 A, b = 76.7 A, c = 127.5 A, complex by Co-crystallization, beta-c-uPA in complex with inhibitor UPA-I4, space group P4(1)2(1)2, cell constants a = 55.0 A, b = 55.0 A, c = 151.6 A, complex by Co-crystallization	Homo sapiens

Crystallization (Comment)

Organism

beta-c-uPA in complex with inhibitor UPA-I1, space group P2(1)2(1)2(1), cell constants a = 53.2 A, b = 54.7 A, c = 82.4 A, beta-c-uPA in complex with inhibitor UPA-I3, space group P2(1)2(1)2(1), cell constants a = 52.9 A, b = 54.7 A, c = 81.4 A, beta-c-uPA in complex with inhibitor UPA-I2, space group P2(1)2(1)2(1), cell constants a = 53.0 A, b = 54.4 A, c = 82.2 A, beta-c-uPA in complex with inhibitor UPA-I5, space group P2(1)2(1)2(1), cell constants a = 53.0 A, b = 54.9 A, c = 82.3 A, beta-c-uPA in complex with inhibitor UPA-I6, space group P2(1)2(1)2(1), cell constants a = 53.5 A, b = 54.8 A, c = 82.4 A, complex by soaking, Ybeta-c-uPA in complex with inhibitor UPA-I6, space group P4(3)2(1)2, cell constants a = 76.7 A, b = 76.7 A, c = 127.5 A, complex by Co-crystallization, beta-c-uPA in complex with inhibitor UPA-I4, space group P4(1)2(1)2, cell constants a = 55.0 A, b = 55.0 A, c = 151.6 A, complex by Co-crystallization

Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
C122S	mutant of the serine proteinase domain	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal	-	Homo sapiens
phenethylsulfonamidino-D-seryl-L-alanyl-L-argininal	-	Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da]	Molecular Weight Maximum [Da]	Comment	Organism
55000	-	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	human	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
L-pyroglutamyl-glycyl-L-arginine-p-nitroanilide + H2O	-	Homo sapiens	L-pyroglutamyl-glycyl-L-arginine + 4-nitroaniline	-	?

Synonyms

Synonyms	Comment	Organism
urokinase type plasminogen activator	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
0.000002	-	phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal	pH 7.4, 37°C, compound uPA-I5	Homo sapiens
0.000003	-	phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal	pH 7.4, 37°C, compound uPA-I6	Homo sapiens
0.000006	-	phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal	pH 7.4, 37°C, compound uPA-I3	Homo sapiens
0.000014	-	phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal	pH 7.4, 37°C, compound uPA-I4	Homo sapiens
0.000021	-	phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal	pH 7.4, 37°C, compound uPA-I1	Homo sapiens
0.000028	-	phenethylsulfonamidino-D-seryl-L-alanyl(P2)-L-argininal	pH 7.4, 37°C, compound uPA-I2	Homo sapiens