Target Information

Target General Infomation
Target ID
T45299
Former ID
TTDR01233
Target Name
Tissue-type plasminogen activator
Gene Name
PLAT
Synonyms
Alteplase; Reteplase; T-PA; T-plasminogen activator; TPA; PLAT
Target Type
Research
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.
BioChemical Class
Peptidase
Target Validation
T45299
UniProt ID
P00750
EC Number
EC 3.4.21.68
Sequence
MDAMKRGLCCVLLLCGAVFVSPSQEIHARFRRGARSYQVICRDEKTQMIYQQHQSWLRPV
LRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCE
IDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCR
NPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWN
SMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCG
LRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQ
ERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCA
QESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQH
LLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQK
DVPGVYTKVTNYLDWIRDNMRP
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 526118J 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 526236Bioorg Med Chem Lett. 2002 Jan 21;12(2):181-4.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.
Ref 527081Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
Ref 528796J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.
Ref 530503Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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