Therapeutic Targets Database
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TTD Target ID: TTDR01233

Target Information
NameTissue-type plasminogen activator    
Type of targetResearch target    
SynonymsAlteplase    
Reteplase    
T-PA    
T-plasminogen activator    
TPA    
DiseaseNeurological diseases    [1]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.21.68
PathwayComplement and coagulation cascades
UniProt IDP00750
PDB Structure1A5H; 1BDA; 1PK2; 1PML; 1RTF; 1TPG; 1TPK; 1TPM.    
FunctionConverts 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.    
SequenceMDAMKRGLCCVLLLCGAVFVSPSQEIHARFRRGARSYQVICRDEKTQMIYQQHQSWLRPV LRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCE IDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCR NPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWN SMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCG LRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQ ERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCA QESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQH LLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQK DVPGVYTKVTNYLDWIRDNMRP
Related US Patent6,541,452
Target ValidationClick to Find Target Validation Information.    
Inhibitor1-guanidino-N-phenyl-7-isoquinolinesulphonamide[2]
2- (2-Hydroxy-phenyl)-1H-indole-5-carboxamidine[3]
5- (DIMETHYLAMINO)-2-NAPHTHALENESULFONIC ACID[4]
6-Amino Hexanoic Acid[5]
BMS-344577[6]
N- (4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine[7]
N- (4-Phenyl-pyridin-2-yl)-guanidine[8]
N- (5-Benzyloxy-isoquinolin-1-yl)-guanidine[7]
N- (7-Benzyloxy-isoquinolin-1-yl)-guanidine[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The effect of epsilon-aminocaproic acid and aprotinin on fibrinolysis and blood loss in patients undergoing primary, isolated coronary artery bypass surgery: a randomized, double-blind, placebo-controlled, noninferiority trial. Anesth Analg. 2009 Jul;109(1):15-24. To Reference
Ref 2J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. To Reference
Ref 3J 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. To Reference
Ref 4Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 5Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 6Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. To Reference
Ref 7Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. To Reference
Ref 8Bioorg Med Chem Lett. 2002 Jan 21;12(2):181-4.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines. To Reference



 

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