DB code: M00152

RLCP classification 1.13.30000.10 : Hydrolysis
CATH domain 2.10.25.10 : Laminin
2.40.20.10 : Plasminogen Kringle 4
2.40.10.10 : Thrombin, subunit H Catalytic domain
2.40.10.10 : Thrombin, subunit H Catalytic domain
E.C. 3.4.21.73
CSA
M-CSA
MACiE

CATH domain Related DB codes (homologues)
2.10.25.10 : Laminin M00139 M00133 M00212 M00155 M00315 M00316
2.40.10.10 : Thrombin, subunit H M00139 D00214 M00167 D00426 M00133 D00428 D00429 D00430 D00431 D00432 D00433 D00434 D00435 M00227 M00209 D00194 D00197 D00211 D00212 D00216 M00212 D00224 D00497 M00217 M00216 D00528 D00848 D00850 D00851 D00852 D00855 M00155 M00157 M00181 M00315 M00316 M00317 M00348 M00349 T00074 T00410 T00411
2.40.20.10 : Plasminogen Kringle 4 M00155 M00157

Uniprot Enzyme Name
UniprotKB Protein name Synonyms Contains RefSeq MEROPS Pfam
P00749 Urokinase-type plasminogen activator
U-plasminogen activator
uPA
EC 3.4.21.73
Urokinase-type plasminogen activator long chain A
Urokinase-type plasminogen activator short chain A
Urokinase-type plasminogen activator chain B
NP_001138503.1 (Protein)
NM_001145031.1 (DNA/RNA sequence)
NP_002649.1 (Protein)
NM_002658.3 (DNA/RNA sequence)
S01.231 (Serine)
PF00051 (Kringle)
PF00089 (Trypsin)
[Graphical View]

KEGG enzyme name
u-plasminogen activator
urokinase
urinary plasminogen activator
cellular plasminogen activator
urokinase-type plasminogen activator
double-chain urokinase-type plasminogen activator
two-chain urokinase-type plasminogen activator
urokinase plasminogen activator
uPA
u-PA
abbokinase
urinary esterase A

UniprotKB: Accession Number Entry name Activity Subunit Subcellular location Cofactor
P00749 UROK_HUMAN Specific cleavage of Arg-|-Val bond in plasminogen to form plasmin. Found in high and low molecular mass forms. Each consists of two chains, A and B. The high molecular mass form contains a long chain A which is cleaved to yield a short chain A. Binds LRP1B, binding is followed by internalization and degradation. Interacts with MRC2. Interacts with PLAUR. Secreted.

KEGG Pathways
Map code Pathways E.C.

Compound table
Substrates Products Intermediates
KEGG-id C00520 C00001 C00471 I00087 I00085 I00086
E.C.
Compound Plasminogen H2O Plasmin Peptidyl-tetrahedral intermediate Acyl-enzyme Tetrahedral intermediate
Type peptide/protein H2O peptide/protein
ChEBI 15377
PubChem 22247451
962
1urkA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1urkA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1kduA Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1c5wB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:ESI Unbound Unbound Unbound
1c5xB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:ESI Unbound Unbound Unbound
1c5yB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:ESP Unbound Unbound Unbound
1c5zB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:BAM Unbound Unbound Unbound
1ejnA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:AGB Unbound Unbound Unbound Unbound
1f5lA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:AMR Unbound Unbound Unbound
1f92A01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:UKP Unbound Unbound Unbound
1fv9A01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:172 Unbound Unbound Unbound
1gi7B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Analogue:120 Unbound Unbound Unbound
1gi8B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:BMZ Unbound Unbound Unbound Unbound
1gi9B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:123 Unbound Unbound Unbound Unbound
1gj7B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:132 Unbound Unbound Unbound Unbound
1gj8B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:133 Unbound Unbound Unbound Unbound
1gj9B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:134 Unbound Unbound Unbound Unbound
1gjaB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:135 Unbound Unbound Unbound Unbound
1gjbB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:130 Unbound Unbound Unbound Unbound
1gjcB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:130 Unbound Unbound Unbound Unbound
1gjdB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:136 Unbound Unbound Unbound Unbound
1lmwB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Transition-state-analogue:GLU-GLY-MAI (chain I)
1lmwD01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Transition-state-analogue:GLU-GLY-MAI (chain J)
1o3pB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:655 Unbound Unbound Unbound Unbound
1owdA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:497 Unbound Unbound Unbound Unbound
1oweA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:675 Unbound Unbound Unbound Unbound
1owhA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:239 Unbound Unbound Unbound Unbound
1owiA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:426 Unbound Unbound Unbound Unbound
1owjA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:155 Unbound Unbound Unbound Unbound
1owkA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Analogue:303 Unbound Unbound Unbound Unbound
1c5wB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1c5xB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1c5yB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1c5zB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1ejnA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1f5lA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1f92A02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1fv9A02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gi7B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gi8B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gi9B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gj7B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gj8B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gj9B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gjaB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gjbB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gjcB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1gjdB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1lmwB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1lmwD02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1o3pB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1owdA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1oweA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1owhA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1owiA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1owjA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound
1owkA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain Unbound Unbound Unbound Unbound Unbound

Reference for Active-site residues
resource references E.C.

Active-site residues
PDB Catalytic residues Cofactor-binding residues Modified residues Main-chain involved in catalysis Comment
1urkA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain
1urkA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain
1kduA Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain
1c5wB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1c5xB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1c5yB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1c5zB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1ejnA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1f5lA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1f92A01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1fv9A01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 197 GLY 193;SER 195
1gi7B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gi8B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gi9B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gj7B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gj8B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gj9B01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gjaB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gjbB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gjcB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1gjdB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1lmwB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1lmwD01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1o3pB01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 195 GLY 193;SER 195
1owdA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 197 GLY 193;SER 195
1oweA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 211 GLY 193;SER 195
1owhA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 211 GLY 193;SER 195
1owiA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 197 GLY 193;SER 195
1owjA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 197 GLY 193;SER 195
1owkA01 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain SER 197 GLY 193;SER 195
1c5wB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1c5xB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1c5yB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1c5zB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1ejnA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1f5lA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1f92A02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1fv9A02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 45;ASP 96
1gi7B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gi8B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gi9B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gj7B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gj8B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gj9B02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gjaB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gjbB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gjcB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1gjdB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1lmwB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1lmwD02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1o3pB02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 57;ASP 102
1owdA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 45;ASP 96
1oweA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 54;ASP 109
1owhA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 54;ASP 109
1owiA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 45;ASP 96
1owjA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 45;ASP 96
1owkA02 Pdbj logo s Rasmollogo id Rasmollogo chain Mmcif id Mmcif chain HIS 45;ASP 96

References for Catalytic Mechanism
References Sections No. of steps in catalysis
[19]
[45]

References
[1]
Resource
Comments
Medline ID
PubMed ID 6498202
Journal Biochim Biophys Acta
Year 1984
Volume 791
Pages 1-8
Authors Miwa N, Sawada T, Suzuki A
Title Conformational changes in human urokinase induced by a specific reduction of disulfide bond in Cys-194-Cys-222 associated with exhibition of enzymatic activity.
Related PDB
Related UniProtKB
[2]
Resource
Comments
Medline ID
PubMed ID 3114883
Journal Semin Thromb Hemost
Year 1987
Volume 13
Pages 152-9
Authors Lijnen HR, Stump DC, Collen DC
Title Single-chain urokinase-type plasminogen activator: mechanism of action and thrombolytic properties.
Related PDB
Related UniProtKB
[3]
Resource
Comments
Medline ID
PubMed ID 3365258
Journal Biochem Biophys Res Commun
Year 1988
Volume 152
Pages 910-5
Authors Charpie JR, Haber E, Matsueda GR
Title A sequence-dependent monoclonal antibody specific for single-chain urokinase.
Related PDB
Related UniProtKB
[4]
Resource
Comments
Medline ID
PubMed ID 2894309
Journal Eur J Biochem
Year 1988
Volume 172
Pages 185-8
Authors Lijnen HR, Van Hoef B, Nelles L, Holmes WE, Collen D
Title Enzymatic properties of single-chain and two-chain forms of a Lys158----Glu158 mutant of urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[5]
Resource
Comments STRUCTURE BY NMR.
Medline ID 89127526
PubMed ID 2536903
Journal Nature
Year 1989
Volume 337
Pages 579-82
Authors Oswald RE, Bogusky MJ, Bamberger M, Smith RA, Dobson CM
Title Dynamics of the multidomain fibrinolytic protein urokinase from two-dimensional NMR.
Related PDB
Related UniProtKB P00749
[6]
Resource
Comments
Medline ID
PubMed ID 1847867
Journal Eur J Biochem
Year 1991
Volume 195
Pages 691-7
Authors Orsini G, Brandazza A, Sarmientos P, Molinari A, Lansen J, Cauet G
Title Efficient renaturation and fibrinolytic properties of prourokinase and a deletion mutant expressed in Escherichia coli as inclusion bodies.
Related PDB
Related UniProtKB
[7]
Resource
Comments STRUCTURE BY NMR OF 67-155.
Medline ID 93003110
PubMed ID 1327118
Journal Biochemistry
Year 1992
Volume 31
Pages 9562-71
Authors Li X, Smith RA, Dobson CM
Title Sequential 1H NMR assignments and secondary structure of the kringle domain from urokinase.
Related PDB 1kdu
Related UniProtKB P00749
[8]
Resource
Comments
Medline ID
PubMed ID 1510944
Journal Biochemistry
Year 1992
Volume 31
Pages 7572-9
Authors Stephens RW, Bokman AM, Myohanen HT, Reisberg T, Tapiovaara H, Pedersen N, Grondahl-Hansen J, Llinas M, Vaheri A
Title Heparin binding to the urokinase kringle domain.
Related PDB
Related UniProtKB
[9]
Resource
Comments
Medline ID
PubMed ID 1310986
Journal J Biol Chem
Year 1992
Volume 267
Pages 3878-85
Authors Novokhatny V, Medved L, Mazar A, Marcotte P, Henkin J, Ingham K
Title Domain structure and interactions of recombinant urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[10]
Resource
Comments
Medline ID
PubMed ID 8380336
Journal Biochemistry
Year 1993
Volume 32
Pages 298-309
Authors Nowak UK, Li X, Teuten AJ, Smith RA, Dobson CM
Title NMR studies of the dynamics of the multidomain protein urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[11]
Resource
Comments
Medline ID
PubMed ID 8314753
Journal J Biol Chem
Year 1993
Volume 268
Pages 13858-68
Authors Bokman AM, Jimenez-Barbero J, Llinas M
Title 1H NMR characterization of the urokinase kringle module. Structural, but not functional, relatedness to homologous domains.
Related PDB
Related UniProtKB
[12]
Resource
Comments
Medline ID
PubMed ID 8449917
Journal J Biol Chem
Year 1993
Volume 268
Pages 5550-6
Authors Lubin IM, Caban R, Runge MS
Title The tissue plasminogen activator finger domain confers fibrin-dependent enhancement of catalytic activity to single-chain urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[13]
Resource
Comments
Medline ID
PubMed ID 7803405
Journal Biochemistry
Year 1994
Volume 33
Pages 15418-24
Authors Hansen AP, Petros AM, Meadows RP, Fesik SW
Title Backbone dynamics of a two-domain protein: 15N relaxation studies of the amino-terminal fragment of urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[14]
Resource
Comments X-ray crystallography
Medline ID
PubMed ID 8161544
Journal Biochemistry
Year 1994
Volume 33
Pages 4847-64
Authors Hansen AP, Petros AM, Meadows RP, Nettesheim DG, Mazar AP, Olejniczak ET, Xu RX, Pederson TM, Henkin J, Fesik SW
Title Solution structure of the amino-terminal fragment of urokinase-type plasminogen activator.
Related PDB 1urk
Related UniProtKB
[15]
Resource
Comments
Medline ID
PubMed ID 8130209
Journal Biochemistry
Year 1994
Volume 33
Pages 2951-60
Authors Nowak UK, Cooper A, Saunders D, Smith RA, Dobson CM
Title Unfolding studies of the protease domain of urokinase-type plasminogen activator: the existence of partly folded states and stable subdomains.
Related PDB
Related UniProtKB
[16]
Resource
Comments STRUCTURE BY NMR OF 67-155.
Medline ID 94149701
PubMed ID 8107091
Journal J Mol Biol
Year 1994
Volume 235
Pages 1548-59
Authors Li X, Bokman AM, Llinas M, Smith RA, Dobson CM
Title Solution structure of the kringle domain from urokinase-type plasminogen activator.
Related PDB
Related UniProtKB P00749
[17]
Resource
Comments
Medline ID
PubMed ID 7548000
Journal Biochemistry
Year 1995
Volume 34
Pages 12524-34
Authors Ploug M, Rahbek-Nielsen H, Ellis V, Roepstorff P, Dano K
Title Chemical modification of the urokinase-type plasminogen activator and its receptor using tetranitromethane. Evidence for the involvement of specific tyrosine residues in both molecules during receptor-ligand interaction.
Related PDB
Related UniProtKB
[18]
Resource
Comments
Medline ID
PubMed ID 8869642
Journal Protein Eng
Year 1995
Volume 8
Pages 1295-1302
Authors Bakker AH, Nieuwenbroek NM, Verheijen JH
Title Domain-domain interactions in hybrids of tissue-type plasminogen activator and urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[19]
Resource
Comments X-RAY CRYSTALLOGRAPHY (2.5 ANGSTROMS).
Medline ID 96000858
PubMed ID 8591045
Journal Structure
Year 1995
Volume 3
Pages 681-91
Authors Spraggon G, Phillips C, Nowak UK, Ponting CP, Saunders D, Dobson CM, Stuart DI, Jones EY
Title The crystal structure of the catalytic domain of human urokinase-type plasminogen activator.
Related PDB 1lmw
Related UniProtKB P00749
[20]
Resource
Comments
Medline ID
PubMed ID 8647121
Journal Eur J Biochem
Year 1996
Volume 237
Pages 743-51
Authors Magdolen V, Rettenberger P, Koppitz M, Goretzki L, Kessler H, Weidle UH, Konig B, Graeff H, Schmitt M, Wilhelm O
Title Systematic mutational analysis of the receptor-binding region of the human urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[21]
Resource
Comments
Medline ID
PubMed ID 9295329
Journal J Biol Chem
Year 1997
Volume 272
Pages 23818-23
Authors Sun Z, Jiang Y, Ma Z, Wu H, Liu BF, Xue Y, Tang W, Chen Y, Li C, Zhu D, Gurewich V, Liu JN, Zhong M, Xu Y
Title Identification of a flexible loop region (297-313) of urokinase-type plasminogen activator, which helps determine its catalytic activity.
Related PDB
Related UniProtKB
[22]
Resource
Comments
Medline ID
PubMed ID 9843416
Journal Biochemistry
Year 1998
Volume 37
Pages 16494-505
Authors Ploug M
Title Identification of specific sites involved in ligand binding by photoaffinity labeling of the receptor for the urokinase-type plasminogen activator. Residues located at equivalent positions in uPAR domains I and III participate in the assembly of a composite ligand-binding site.
Related PDB
Related UniProtKB
[23]
Resource
Comments
Medline ID
PubMed ID 9521680
Journal Biochemistry
Year 1998
Volume 37
Pages 3612-22
Authors Ploug M, Ostergaard S, Hansen LB, Holm A, Dano K
Title Photoaffinity labeling of the human receptor for urokinase-type plasminogen activator using a decapeptide antagonist. Evidence for a composite ligand-binding site and a short interdomain separation.
Related PDB
Related UniProtKB
[24]
Resource
Comments
Medline ID
PubMed ID 9485445
Journal Biochemistry
Year 1998
Volume 37
Pages 2935-40
Authors Sun Z, Liu BF, Chen Y, Gurewich V, Zhu D, Liu JN
Title Analysis of the forces which stabilize the active conformation of urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[25]
Resource
Comments
Medline ID
PubMed ID 9804393
Journal Clin Chem Lab Med
Year 1998
Volume 36
Pages 697-702
Authors Orgel D, Schroder W, Hecker-Kia A, Weithmann KU, Kolkenbrock H, Ulbrich N
Title The cleavage of pro-urokinase type plasminogen activator by stromelysin-1.
Related PDB
Related UniProtKB
[26]
Resource
Comments
Medline ID
PubMed ID 9760182
Journal Eur J Biochem
Year 1998
Volume 256
Pages 411-8
Authors Oda M, Shiraishi A, Hasegawa M
Title Analysis of the ternary complex formation of human urokinase with the separated two domains of its receptor.
Related PDB
Related UniProtKB
[27]
Resource
Comments
Medline ID
PubMed ID 10540331
Journal Eur J Immunol
Year 1999
Volume 29
Pages 3196-209
Authors Olivier P, Bieler G, Muller KM, Hauzenberger D, Ruegg C
Title Urokinase-type plasminogen activator inhibits alpha 4 beta 1 integrin-mediated T lymphocyte adhesion to fibronectin independently of its catalytic activity.
Related PDB
Related UniProtKB
[28]
Resource
Comments X-ray crystallography
Medline ID
PubMed ID 10779411
Journal Chem Biol
Year 2000
Volume 7
Pages 299-312
Authors Katz BA, Mackman R, Luong C, Radika K, Martelli A, Sprengeler PA, Wang J, Chan H, Wong L
Title Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.
Related PDB 1c5w 1c5x 1c5y 1c5z
Related UniProtKB
[29]
Resource
Comments X-ray crystallography
Medline ID
PubMed ID 10926521
Journal J Mol Biol
Year 2000
Volume 301
Pages 465-75
Authors Zeslawska E, Schweinitz A, Karcher A, Sondermann P, Sperl S, Sturzebecher J, Jacob U
Title Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design.
Related PDB 1f5l 1f92
Related UniProtKB
[30]
Resource
Comments X-RAY CRYSTALLOGRAPHY (1.8 ANGSTROMS) OF 159-411.
Medline ID 20266327
PubMed ID 10805774
Journal Proc Natl Acad Sci U S A
Year 2000
Volume 97
Pages 5113-8
Authors Sperl S, Jacob U, Arroyo de Prada N, Sturzebecher J, Wilhelm OG, Bode W, Magdolen V, Huber R, Moroder L
Title (4-aminomethyl)phenylguanidine derivatives as nonpeptidic highly selective inhibitors of human urokinase.
Related PDB 1ejn
Related UniProtKB P00749
[31]
Resource
Comments
Medline ID
PubMed ID 11150590
Journal Thromb Res
Year 2000
Volume 100
Pages 461-7
Authors Wang P, Zhang J, Sun Z, Chen Y, Gurewich V, Liu JN
Title Catalytic and fibrinolytic properties of recombinant urokinase plasminogen activator from E. coli, mammalian, and yeast cells.
Related PDB
Related UniProtKB
[32]
Resource
Comments X-ray crystallography
Medline ID
PubMed ID 11731301
Journal Chem Biol
Year 2001
Volume 8
Pages 1107-21
Authors Katz BA, Sprengeler PA, Luong C, Verner E, Elrod K, Kirtley M, Janc J, Spencer JR, Breitenbucher JG, Hui H, McGee D, Allen D, Martelli A, Mackman RL
Title Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.
Related PDB 1gj7 1gj8 1gj9 1gja 1gjb 1gjc 1gjd
Related UniProtKB
[33]
Resource
Comments
Medline ID
PubMed ID 11562773
Journal Int J Mol Med
Year 2001
Volume 8
Pages 365-71
Authors Jankun J, Skrzypczak-Jankun E
Title Binding site of amiloride to urokinase plasminogen activator depends on species.
Related PDB
Related UniProtKB
[34]
Resource
Comments
Medline ID
PubMed ID 11689072
Journal J Med Chem
Year 2001
Volume 44
Pages 3856-71
Authors Mackman RL, Katz BA, Breitenbucher JG, Hui HC, Verner E, Luong C, Liu L, Sprengeler PA
Title Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[35]
Resource
Comments
Medline ID
PubMed ID 11495587
Journal J Med Chem
Year 2001
Volume 44
Pages 2753-71
Authors Verner E, Katz BA, Spencer JR, Allen D, Hataye J, Hruzewicz W, Hui HC, Kolesnikov A, Li Y, Luong C, Martelli A, Radika K, Rai R, She M, Shrader W, Sprengeler PA, Trapp S, Wang J, Young WB, Mackman RL
Title Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.
Related PDB
Related UniProtKB
[36]
Resource
Comments X-ray crystallography
Medline ID
PubMed ID 11292354
Journal J Mol Biol
Year 2001
Volume 307
Pages 1451-86
Authors Katz BA, Elrod K, Luong C, Rice MJ, Mackman RL, Sprengeler PA, Spencer J, Hataye J, Janc J, Link J, Litvak J, Rai R, Rice K, Sideris S, Verner E, Young W
Title A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.
Related PDB 1gi7 1gi8 1gi9
Related UniProtKB
[37]
Resource
Comments
Medline ID
PubMed ID 11841346
Journal Biochemistry (Mosc)
Year 2002
Volume 67
Pages 109-18
Authors Stepanova VV, Tkachuk VA
Title Urokinase as a multidomain protein and polyfunctional cell regulator.
Related PDB
Related UniProtKB
[38]
Resource
Comments
Medline ID
PubMed ID 12113832
Journal Bioorg Med Chem Lett
Year 2002
Volume 12
Pages 2019-22
Authors Mackman RL, Hui HC, Breitenbucher JG, Katz BA, Luong C, Martelli A, McGee D, Radika K, Sendzik M, Spencer JR, Sprengeler PA, Tario J, Verner E, Wang J
Title 2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.
Related PDB
Related UniProtKB
[39]
Resource
Comments
Medline ID
PubMed ID 12113833
Journal Bioorg Med Chem Lett
Year 2002
Volume 12
Pages 2023-6
Authors Spencer JR, McGee D, Allen D, Katz BA, Luong C, Sendzik M, Squires N, Mackman RL
Title 4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.
Related PDB
Related UniProtKB
[40]
Resource
Comments
Medline ID
PubMed ID 12369939
Journal Curr Pharm Des
Year 2002
Volume 8
Pages 2541-58
Authors Rockway TW, Nienaber V, Giranda VL
Title Inhibitors of the protease domain of urokinase-type plasminogen activator.
Related PDB
Related UniProtKB
[41]
Resource
Comments
Medline ID
PubMed ID 12408709
Journal J Med Chem
Year 2002
Volume 45
Pages 4984-94
Authors Schmiedeberg N, Schmitt M, Rolz C, Truffault V, Sukopp M, Burgle M, Wilhelm OG, Schmalix W, Magdolen V, Kessler H
Title Synthesis, solution structure, and biological evaluation of urokinase type plasminogen activator (uPA)-derived receptor binding domain mimetics.
Related PDB
Related UniProtKB
[42]
Resource
Comments
Medline ID
PubMed ID 12182908
Journal Thromb Res
Year 2002
Volume 106
Pages 105-11
Authors Sun Z, Zhang PX, Wang P, Gurewich V, Shen HY, Liu JN
Title Amino-terminal fragment of urokinase-type plasminogen activator inhibits its plasminogen activation.
Related PDB
Related UniProtKB
[43]
Resource
Comments
Medline ID
PubMed ID 12675515
Journal Biol Chem
Year 2003
Volume 384
Pages 229-36
Authors Liang OD, Chavakis T, Linder M, Bdeir K, Kuo A, Preissner KT
Title Binding of urokinase plasminogen activator to gp130 via a putative urokinase-binding consensus sequence.
Related PDB
Related UniProtKB
[44]
Resource
Comments
Medline ID
PubMed ID 12529357
Journal J Biol Chem
Year 2003
Volume 278
Pages 11449-56
Authors Kim KS, Hong YK, Joe YA, Lee Y, Shin JY, Park HE, Lee IH, Lee SY, Kang DK, Chang SI, Chung SI
Title Anti-angiogenic activity of the recombinant kringle domain of urokinase and its specific entry into endothelial cells.
Related PDB
Related UniProtKB
[45]
Resource
Comments X-ray crystallography
Medline ID
PubMed ID 12742021
Journal J Mol Biol
Year 2003
Volume 329
Pages 93-120
Authors Katz BA, Elrod K, Verner E, Mackman RL, Luong C, Shrader WD, Sendzik M, Spencer JR, Sprengeler PA, Kolesnikov A, Tai VW, Hui HC, Breitenbucher JG, Allen D, Janc JW
Title Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.
Related PDB 1o3p
Related UniProtKB
[46]
Resource
Comments
Medline ID
PubMed ID 12684001
Journal J Mol Biol
Year 2003
Volume 328
Pages 109-18
Authors Zeslawska E, Jacob U, Schweinitz A, Coombs G, Bode W, Madison E
Title Crystals of urokinase type plasminogen activator complexes reveal the binding mode of peptidomimetic inhibitors.
Related PDB
Related UniProtKB
[47]
Resource
Comments X-ray crystallography
Medline ID
PubMed ID 14711304
Journal J Med Chem
Year 2004
Volume 47
Pages 303-24
Authors Wendt MD, Rockway TW, Geyer A, McClellan W, Weitzberg M, Zhao X, Mantei R, Nienaber VL, Stewart K, Klinghofer V, Giranda VL
Title Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.
Related PDB 1owd 1owe 1owh 1owi 1owj 1owk
Related UniProtKB

Comments
This enzyme is composed of the N-terminal EGF-like domain (corresponding to 1urk), Kringle one (corresponding to 1urk & 1kdu) and serine protease ones. This enzyme belongst to the peptidase family-S1. It has a classic catalytic triad (ser/His/Asp), suggesting that it has a similar catalytic mechanism to that of other serine proteases, such as trypsin (D00197 in EzCatDB).

Created Updated
2004-11-09 2011-02-21