Target Information
Target General Infomation | |||||
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Target ID |
T45299
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Former ID |
TTDR01233
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Target Name |
Tissue-type plasminogen activator
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Gene Name |
PLAT
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Synonyms |
Alteplase; Reteplase; T-PA; T-plasminogen activator; TPA; PLAT
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Target Type |
Research
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Function |
Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a single arg-val bond in plasminogen. By controlling plasmin-mediated proteolysis, it plays an important role in tissue remodeling and degradation and in cell migration.
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BioChemical Class |
Peptidase
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Target Validation |
T45299
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UniProt ID | |||||
EC Number |
EC 3.4.21.68
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Sequence |
MDAMKRGLCCVLLLCGAVFVSPSQEIHARFRRGARSYQVICRDEKTQMIYQQHQSWLRPV
LRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCE IDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCR NPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWN SMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCG LRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQ ERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCA QESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQH LLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQK DVPGVYTKVTNYLDWIRDNMRP |
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Inhibitor | 1-guanidino-N-phenyl-7-isoquinolinesulphonamide | Drug Info | [528796] | ||
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine | Drug Info | [526118] | |||
5-(DIMETHYLAMINO)-2-NAPHTHALENESULFONIC ACID | Drug Info | [551374] | |||
6-Amino Hexanoic Acid | Drug Info | [551393] | |||
BMS-344577 | Drug Info | [530503] | |||
N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine | Drug Info | [527081] | |||
N-(4-Phenyl-pyridin-2-yl)-guanidine | Drug Info | [526236] | |||
N-(5-Benzyloxy-isoquinolin-1-yl)-guanidine | Drug Info | [527081] | |||
N-(7-Benzyloxy-isoquinolin-1-yl)-guanidine | Drug Info | [527081] | |||
Pathways | |||||
KEGG Pathway | Complement and coagulation cascades | ||||
Transcriptional misregulation in cancer | |||||
NetPath Pathway | IL5 Signaling Pathway | ||||
PANTHER Pathway | Blood coagulation | ||||
Plasminogen activating cascade | |||||
Pathway Interaction Database | amb2 Integrin signaling | ||||
Beta2 integrin cell surface interactions | |||||
PathWhiz Pathway | Coagulation | ||||
Reactome | Dissolution of Fibrin Clot | ||||
WikiPathways | Senescence and Autophagy in Cancer | ||||
Complement and Coagulation Cascades | |||||
Endochondral Ossification | |||||
Blood Clotting Cascade | |||||
Dissolution of Fibrin Clot | |||||
Folate Metabolism | |||||
Vitamin B12 Metabolism | |||||
Selenium Micronutrient Network | |||||
References | |||||
Ref 526118 | J Med Chem. 2001 Aug 16;44(17):2753-71.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. | ||||
Ref 526236 | Bioorg Med Chem Lett. 2002 Jan 21;12(2):181-4.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines. | ||||
Ref 527081 | Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. | ||||
Ref 528796 | J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. |
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