Therapeutic Targets Database
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TTD Target ID: TTDC00312

Target Information
NameUrokinase-type plasminogen activator    
Type of targetClinical trial target    
SynonymsU-plasminogen activator    
UPA    
DiseaseCancer, unspecific    [1][2]
Melanoma    [3]
Drug(s)AmediplasePhase IIIThrombolysis[4]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.21.73
PathwayComplement and coagulation cascades
UniProt IDP00749
PDB Structure1C5W; 1C5X; 1C5Y; 1C5Z; 1EJN; 1F5K; 1F5L; 1F92.    
FunctionPotent plasminogen activator and is clinically used for therapy of thrombolytic disorders.    
SequenceMRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQ HCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHN YCRNPDNRRRPWCYVQVGLKPLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKII GGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLMSPCWVISATHCFIDYPKKEDYIVYLG RSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICL PSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKML CAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIR SHTKEENGLAL
Related US Patent6,207,701
6,248,738
6,274,619
6,465,503
6,495,562
6,504,031
6,528,619
6,562,840
6,583,162
6,624,169
6,673,789
6,680,320
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2R)-1-[5]
(3,4-dichlorophenyl)[6]
(3-nitro-1H-pyrazol-1-yl)[6]
(4-bromo-1H-pyrazol-1-yl)[6]
(4-guanidino-benzyl)-carbamic acid benzyl ester[7]
(4-nitro-1H-pyrazol-1-yl)[6]
(4-nitro-1H-pyrazol-1-yl)[6]
1-[4- (2-oxo-2-phenylethyl)phenyl]guanidine[5]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide[6]
1-guanidino-7-isoquinolinesulphonamide[8]
1-guanidino-N-phenyl-7-isoquinolinesulphonamide[8]
2- (2-Hydroxy-phenyl)-1H-indole-5-carboxamidine[9]
2-Amino-5-Hydroxy-Benzimidazole[10]
2-nas-phe (3-am)-4-[11]
4-Iodo-benzo[b]thiophene-2-carboxamidine[12]
4-Iodobenzo[B]Thiophene-2-Carboxamidine[5]
4-chloro-1-guanidino-7-isoquinolinesulphonamide[8]
4-iodobenzo[b]thiophene 2-carboxamidine[13]
4-methoxy-N'- (2-phenylacetyl)benzohydrazide[6]
5-Methylsulfanyl-thiophene-2-carboxamidine[12]
6- (N-Phenylcarbamyl)-2-Naphthalenecarboxamidine[10]
Benzamidine[10]
CRA_10655[5]
CRA_8696[5]
Fucose[10]
N- (1-Adamantyl)-N'-[10]
PAI-1[14]
PAI-2[15]
Thieno[2,3-B]Pyridine-2-Carboxamidine[5]
ActivatorAmediplase[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Clinical utility of urokinase-type plasminogen activator and plasminogen activator inhibitor-1 determination in primary breast cancer tissue for individualized therapy concepts. Clin Breast Cancer. 2002 Aug;3(3):196-200. To Reference
Ref 2Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite. Structure. 2000 May 15;8(5):553-63. To Reference
Ref 3Expression of plasminogen activators and plasminogen activator inhibitors in cutaneous melanomas of transgenic melanoma-susceptible mice. Cancer Res. 1995 Oct 15;55(20):4681-7. To Reference
Ref 4Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. To Reference
Ref 5Berman 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 6J Med Chem. 2007 Oct 4;50(20):4928-38. Epub 2007 Sep 12.N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase. To Reference
Ref 7J Med Chem. 2007 Dec 27;50(26):6638-46. Epub 2007 Dec 1.Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties. To Reference
Ref 8J 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 9J 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 10Overington 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 11J Med Chem. 2006 Jul 13;49(14):4116-26.Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase. To Reference
Ref 12Bioorg Med Chem Lett. 2002 Feb 11;12(3):491-5.Design and synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors. To Reference
Ref 13Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator. Chem Biol. 2000 Apr;7(4):299-312. To Reference
Ref 14Urokinase-type plasminogen activator and its inhibitor PAI-1: predictors of poor response to tamoxifen therapy in recurrent breast cancer. J Natl Cancer Inst. 1995 May 17;87(10):751-6. To Reference
Ref 15Topological localization of plasminogen activator inhibitor type 2. Cytometry. 2000 May 1;40(1):32-41. To Reference



 

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