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 15377 |
||||||||||
| PubChem |
22247451 962 22247451 962 |
||||||||||
| 1urkA01 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1urkA02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1kduA |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1c5wB01 |
|
|
|
|
|
Unbound | Analogue:ESI | Unbound | Unbound | Unbound | |
| 1c5xB01 |
|
|
|
|
|
Unbound | Analogue:ESI | Unbound | Unbound | Unbound | |
| 1c5yB01 |
|
|
|
|
|
Unbound | Analogue:ESP | Unbound | Unbound | Unbound | |
| 1c5zB01 |
|
|
|
|
|
Unbound | Analogue:BAM | Unbound | Unbound | Unbound | |
| 1ejnA01 |
|
|
|
|
|
Analogue:AGB | Unbound | Unbound | Unbound | Unbound | |
| 1f5lA01 |
|
|
|
|
|
Unbound | Analogue:AMR | Unbound | Unbound | Unbound | |
| 1f92A01 |
|
|
|
|
|
Unbound | Analogue:UKP | Unbound | Unbound | Unbound | |
| 1fv9A01 |
|
|
|
|
|
Unbound | Analogue:172 | Unbound | Unbound | Unbound | |
| 1gi7B01 |
|
|
|
|
|
Unbound | Analogue:120 | Unbound | Unbound | Unbound | |
| 1gi8B01 |
|
|
|
|
|
Analogue:BMZ | Unbound | Unbound | Unbound | Unbound | |
| 1gi9B01 |
|
|
|
|
|
Analogue:123 | Unbound | Unbound | Unbound | Unbound | |
| 1gj7B01 |
|
|
|
|
|
Analogue:132 | Unbound | Unbound | Unbound | Unbound | |
| 1gj8B01 |
|
|
|
|
|
Analogue:133 | Unbound | Unbound | Unbound | Unbound | |
| 1gj9B01 |
|
|
|
|
|
Analogue:134 | Unbound | Unbound | Unbound | Unbound | |
| 1gjaB01 |
|
|
|
|
|
Analogue:135 | Unbound | Unbound | Unbound | Unbound | |
| 1gjbB01 |
|
|
|
|
|
Analogue:130 | Unbound | Unbound | Unbound | Unbound | |
| 1gjcB01 |
|
|
|
|
|
Analogue:130 | Unbound | Unbound | Unbound | Unbound | |
| 1gjdB01 |
|
|
|
|
|
Analogue:136 | Unbound | Unbound | Unbound | Unbound | |
| 1lmwB01 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Transition-state-analogue:GLU-GLY-MAI (chain I) | |
| 1lmwD01 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Transition-state-analogue:GLU-GLY-MAI (chain J) | |
| 1o3pB01 |
|
|
|
|
|
Analogue:655 | Unbound | Unbound | Unbound | Unbound | |
| 1owdA01 |
|
|
|
|
|
Analogue:497 | Unbound | Unbound | Unbound | Unbound | |
| 1oweA01 |
|
|
|
|
|
Analogue:675 | Unbound | Unbound | Unbound | Unbound | |
| 1owhA01 |
|
|
|
|
|
Analogue:239 | Unbound | Unbound | Unbound | Unbound | |
| 1owiA01 |
|
|
|
|
|
Analogue:426 | Unbound | Unbound | Unbound | Unbound | |
| 1owjA01 |
|
|
|
|
|
Analogue:155 | Unbound | Unbound | Unbound | Unbound | |
| 1owkA01 |
|
|
|
|
|
Analogue:303 | Unbound | Unbound | Unbound | Unbound | |
| 1c5wB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1c5xB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1c5yB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1c5zB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1ejnA02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1f5lA02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1f92A02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1fv9A02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gi7B02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gi8B02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gi9B02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gj7B02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gj8B02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gj9B02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gjaB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gjbB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gjcB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1gjdB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1lmwB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1lmwD02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1o3pB02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1owdA02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1oweA02 |
|
|
|
|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1owhA02 |
|
|
|
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|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1owiA02 |
|
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|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1owjA02 |
|
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|
|
Unbound | Unbound | Unbound | Unbound | Unbound | |
| 1owkA02 |
|
|
|
|
|
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 |
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|||||
| 1urkA02 |
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| 1kduA |
|
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|||||
| 1c5wB01 |
|
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SER 195 | GLY 193;SER 195 | |||
| 1c5xB01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1c5yB01 |
|
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SER 195 | GLY 193;SER 195 | |||
| 1c5zB01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1ejnA01 |
|
|
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SER 195 | GLY 193;SER 195 | |||
| 1f5lA01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1f92A01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1fv9A01 |
|
|
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|
SER 197 | GLY 193;SER 195 | |||
| 1gi7B01 |
|
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1gi8B01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1gi9B01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1gj7B01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1gj8B01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1gj9B01 |
|
|
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|
|
SER 195 | GLY 193;SER 195 | |||
| 1gjaB01 |
|
|
|
|
|
SER 195 | GLY 193;SER 195 | |||
| 1gjbB01 |
|
|
|
|
|
SER 195 | GLY 193;SER 195 | |||
| 1gjcB01 |
|
|
|
|
|
SER 195 | GLY 193;SER 195 | |||
| 1gjdB01 |
|
|
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1lmwB01 |
|
|
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1lmwD01 |
|
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SER 195 | GLY 193;SER 195 | |||
| 1o3pB01 |
|
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|
SER 195 | GLY 193;SER 195 | |||
| 1owdA01 |
|
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|
SER 197 | GLY 193;SER 195 | |||
| 1oweA01 |
|
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SER 211 | GLY 193;SER 195 | |||
| 1owhA01 |
|
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|
SER 211 | GLY 193;SER 195 | |||
| 1owiA01 |
|
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|
SER 197 | GLY 193;SER 195 | |||
| 1owjA01 |
|
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|
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|
SER 197 | GLY 193;SER 195 | |||
| 1owkA01 |
|
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|
SER 197 | GLY 193;SER 195 | |||
| 1c5wB02 |
|
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|
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|
HIS 57;ASP 102 | ||||
| 1c5xB02 |
|
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HIS 57;ASP 102 | ||||
| 1c5yB02 |
|
|
|
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|
HIS 57;ASP 102 | ||||
| 1c5zB02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1ejnA02 |
|
|
|
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|
HIS 57;ASP 102 | ||||
| 1f5lA02 |
|
|
|
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|
HIS 57;ASP 102 | ||||
| 1f92A02 |
|
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HIS 57;ASP 102 | ||||
| 1fv9A02 |
|
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HIS 45;ASP 96 | ||||
| 1gi7B02 |
|
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HIS 57;ASP 102 | ||||
| 1gi8B02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1gi9B02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1gj7B02 |
|
|
|
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HIS 57;ASP 102 | ||||
| 1gj8B02 |
|
|
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|
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HIS 57;ASP 102 | ||||
| 1gj9B02 |
|
|
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HIS 57;ASP 102 | ||||
| 1gjaB02 |
|
|
|
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|
HIS 57;ASP 102 | ||||
| 1gjbB02 |
|
|
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|
|
HIS 57;ASP 102 | ||||
| 1gjcB02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1gjdB02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1lmwB02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1lmwD02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1o3pB02 |
|
|
|
|
|
HIS 57;ASP 102 | ||||
| 1owdA02 |
|
|
|
|
|
HIS 45;ASP 96 | ||||
| 1oweA02 |
|
|
|
|
|
HIS 54;ASP 109 | ||||
| 1owhA02 |
|
|
|
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|
HIS 54;ASP 109 | ||||
| 1owiA02 |
|
|
|
|
|
HIS 45;ASP 96 | ||||
| 1owjA02 |
|
|
|
|
|
HIS 45;ASP 96 | ||||
| 1owkA02 |
|
|
|
|
|
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. |
| 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. |
| 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, |
| 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. |
| 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. |
| 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, |
| 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. |
| 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, |
| 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, |
| 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), |
| Created | Updated |
|---|---|
| 2004-11-09 | 2011-02-21 |