Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00086

Target Information
NameThromboxane-A synthase    
Type of targetClinical trial target    
SynonymsTS    
TXA synthase    
TXS    
Thromboxane A2 synthase    
DiseaseAsthma
[ICD9: 493   ICD10: J45]
[1]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[2]
Cerebral circulatory disorders[1]
Inflammatory Bowel Disease
[ICD9: 555, 556   ICD10: K50, K51]
[3][4]
Ischemic heart disease
[ICD9: 410-414   ICD10: I20-I25]
[1]
Peripheral Vascular Disease
[ICD9: 443.9   ICD10: I73.9]
[5][6][7]
Thromboembolic disorders
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[1]
Drug(s)NM-702Phase IIb completedPeripheral Vascular Disease[7]
NV-52Suspended in Phase IIInflammatory Bowel Disease[3][4]
BioChemical ClassIntramolecular oxidoreductases    
EC NumberEC 5.3.99.5
PathwayArachidonic acid metabolism
Metabolic pathways
UniProt IDP24557
SequenceMEALGFLKLEVNGPMVTVALSVALLALLKWYSTSAFSRLEKLGLRHPKPSPFIGNLTFFR QGFWESQMELRKLYGPLCGYYLGRRMFIVISEPDMIKQVLVENFSNFTNRMASGLEFKSV ADSVLFLRDKRWEEVRGALMSAFSPEKLNEMVPLISQACDLLLAHLKRYAESGDAFDIQR CYCNYTTDVVASVPFGTPVDSWQAPEDPFVKHCKRFFEFCIPRPILVLLLSFPSIMVPLA RILPNKNRDELNGFFNKLIRNVIALRDQQAAEERRRDFLQMVLDARHSASPMGVQDFDIV RDVFSSTGCKPNPSRQHQPSPMARPLTVDEIVGQAFIFLIAGYEIITNTLSFATYLLATN PDCQEKLLREVDVFKEKHMAPEFCSLEEGLPYLDMVIAETLRMYPPAFRFTREAAQDCEV LGQRIPAGAVLEMAVGALHHDPEHWPSPETFNPERFTAEARQQHRPFTYLPFGAGPRSCL GVRLGLLEVKLTLLHVLHKFRFQACPETQVPLQLESKSALGPKNGVYIKIVSR
Target ValidationClick to Find Target Validation Information.    
Inhibitor2- (10-Imidazol-1-yl-decyl)-isoindole-1,3-dione[8]
2- (6-Imidazol-1-yl-hexyl)-isoindole-1,3-dione[8]
2- (8-Imidazol-1-yl-octyl)-isoindole-1,3-dione[8]
4-Methyl-pyridine[9]
5- (2-Imidazol-1-yl-ethyl)-7,8-dihydro-quinoline[10]
5-Imidazol-1-yl-5,6,7,8-tetrahydro-quinoline[10]
6-Imidazol-1-yl-isoquinoline[10]
CGS-13080[11]
CGS-22652[12]
Dazoxiben[13]
Dazoxiben[14]
NM-702[7]
NV-52[3][4]
ONO-1581[15]
Ozagrel[1]
Ozagrel hydrochloride[1]
PYRIDINE[9]
MultitargetNM-702[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Research and development of ozagrel, a highly selective inhibitor of TXA2 synthase. Yakugaku Zasshi. 1994 Dec;114(12):911-33. To Reference
Ref 2Thromboxane A2 and prevention of cardiovascular diseases. Z Kardiol. 1992;81 Suppl 4:185-9. To Reference
Ref 3Phase Ib single- and multiple-dose pharmacokinetic study of oral NV-52 in healthy volunteers. Drugs R D. 2008;9(3):159-66. To Reference
Ref 4Expert Opin Investig Drugs. 2007 Aug;16(8):1255-66.Nv-52: a novel thromboxane synthase inhibitor for the treatment of inflammatory bowel disease. To Reference
Ref 5J Physiol Sci. 2008 Aug;58(4):229-37. Epub 2008 Jun 18.NT-702, a selective phosphodiesterase 3 inhibitor, dilates rabbit spinal arterioles via endothelium-dependent and endothelium-independent mechanisms. To Reference
Ref 6Life Sci. 2007 Sep 1;81(12):970-8. Epub 2007 Aug 8.NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase inhibitor, improves reduced walking distance and lowered hindlimb plantar surface temperature in a rat experimental intermittent claudication model. To Reference
Ref 7The novel phosphodiesterase inhibitor NM-702 improves claudication-limited exercise performance in patients with peripheral arterial disease. J Am Coll Cardiol. 2006 Dec 19;48(12):2539-45. Epub 2006 Nov 28. To Reference
Ref 8J Med Chem. 1986 May;29(5):816-9.Thromboxane synthetase inhibitors and antihypertensive agents. 2. N-[(1H-imidazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones and N-[(1H-1,2,4-triazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones as unique antihypertensive agents. To Reference
Ref 9J Med Chem. 1981 Oct;24(10):1149-55.Highly selective inhibitors of thromboxane synthetase. 2. Pyridine derivatives. To Reference
Ref 10J Med Chem. 2000 May 4;43(9):1841-51.1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase. To Reference
Ref 11J Med Chem. 1985 Feb;28(2):164-70.Imidazo[1,5-a]pyridines: a new class of thromboxane A2 synthetase inhibitors. To Reference
Ref 12Bioorg. Med. Chem. Lett. 4(17):2067-2072 (1994) To Reference
Ref 13Metabolic protection of the reperfused canine endocardium by the thromboxane synthetase inhibitor, dazoxiben. Prostaglandins Leukot Essent Fatty Acids. 1988 Jul;33(1):13-22. To Reference
Ref 14Overington 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 15Bioorg. Med. Chem. Lett. 5(10):1087-1090 (1995) To Reference



 

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