Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00130

Target Information
NameTryptase    
Type of targetSuccessful target    
DiseaseAllergic airway inflammation
[ICD9: 460-519, 995.3   ICD10: J00-J99, T78.4]
[1][2]
Asthma
[ICD9: 493   ICD10: J45]
[2]
Coagulative disorders
[ICD9: 286   ICD10: D65-D69]
[3]
Conjunctivitis
[ICD9: 372.0   ICD10: H10]
[4]
Mast cell-mediated diseases[4]
Rhinitis
[ICD9: 472.0, 477   ICD10: J00, J30, J31.0]
[4]
Drug(s)PentamidineApprovedFungal infections[4][5]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.21.59
Related US Patent6,469,036
6,489,327
6,613,769
6,630,505
6,642,252
6,673,786
Target ValidationClick to Find Target Validation Information.    
InhibitorAMG-126737[2]
APC-366[4]
Actoferrin[4]
BABIM[4]
BMS-262084[6]
GRASSYSTATIN A[7]
Lactoferrin[4]
MOL 6131[2]
Pentamidine[4][5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Inhibitors of tryptase as mast cell-stabilizing agents in the human airways: effects of tryptase and other agonists of proteinase-activated receptor 2 on histamine release. J Pharmacol Exp Ther. 2004 Apr;309(1):119-26. Epub 2004 Jan 13. To Reference
Ref 2Tryptase inhibition blocks airway inflammation in a mouse asthma model. J Immunol. 2002 Feb 15;168(4):1992-2000. To Reference
Ref 3Two-chain factor VIIa generated in the pericardium during surgery with cardiopulmonary bypass : relationship to increased thrombin generation and heparin concentration. Arterioscler Thromb Vasc Biol. 1999 Feb;19(2):248-54. To Reference
Ref 4Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96. To Reference
Ref 5Bis(5-amidino-2-benzimidazolyl)methane and related amidines are potent, reversible inhibitors of mast cell tryptases. J Pharmacol Exp Ther. 1993 Feb;264(2):676-82. To Reference
Ref 6Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. To Reference
Ref 7J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. To Reference



 

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