Therapeutic Targets Database
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TTD Target ID: TTDS00282

Target Information
NameTrypsin    
Type of targetSuccessful target    
SynonymsTrypsinogen    
DiseaseChronic tendon injury[1]
Hemorrhage[2]
Pancreatitis
[ICD9: 577.0-577.1   ICD10: K85, K86.0K86.1]
[3]
Drug(s)AprotininApprovedPerioperative blood loss[4][5]
DermolastinPhase IIAtopic Dermatitis, Alpha 1 Antitrypsin Deficiency[6][7][8][9]
DermolastinHalted in Phase IChronic Obstructive Pulmonary Disease[6][7][8][9]
DermolastinHalted in Phase IEmphysema[6][7][8][9]
EC NumberEC 3.4.21.4
Related US Patent6,583,177
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,3-Di-p-tolyl-[1,3]diazetidine-2,4-dione[10]
1,3-Dibenzyl-[1,3]diazetidine-2,4-dione[10]
1- (3-Amino-benzyl)-1H-indole-5-carboxamidine[11]
1- (3-Nitro-benzyl)-1H-indole-5-carboxamidine[11]
1-Benzyl-1H-indole-5-carboxamidine[11]
2- (2-Hydroxy-phenyl)-1H-indole-5-carboxamidine[12]
2- (2-Iodo-phenyl)-benzo[d][1,3]oxazin-4-one[13]
2-Propionyl-1H-indole-6-carboxamidine[11]
4- (3,4-Diethoxy-benzylamino)-benzamidine[14]
4- (4-Benzyloxy-3-methoxy-benzylamino)-benzamidine[14]
4- (5-Nitro-indol-1-ylmethyl)-benzamidine[11]
4-Indol-1-ylmethyl-benzamidine[11]
6-Styryl-naphthalene-2-carboxamidine[15]
8-Bromo-6-styryl-naphthalene-2-carboxamidine[15]
8-Furan-3-yl-6-styryl-naphthalene-2-carboxamidine[15]
Aprotinin[4][5]
BMY-44621[16]
Benzamidine[17]
Benzamidrazone analogue[18]
Benzamidrazone analogue[18]
Benzamidrazone analogue[18]
Benzamidrazone analogue[18]
Benzamidrazone analogue[18]
Benzamidrazone analogue[18]
Benzamidrazone analogue[18]
CVS-2139[19]
CVS-2359[19]
Dermolastin[6][7][8][9]
GR-133686[20]
GRASSYSTATIN A[21]
INOGATRAN[22]
L-370518[23]
L-371912[23]
L-375378[24]
MELAGATRAN[25]
P1 argininal derivative[26]
P1 argininal derivative[26]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Peptide boronate[27]
Piperidine-1-carboxamidine[28]
RWJ-50353[29]
RWJ-56423[30]
YM-60828[31]
ZK-807834[32]
macrocyclic tripeptide motif[33]
tert-butyloxy carbonyl-D-Phe-pro-Arg-H[34]
MultitargetDermolastin[6][7][8][9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Reducing Extracellular pH Sensitizes the Acinar Cell to Secretagogue-Induced Pancreatitis Responses in Rats. Gastroenterology. 2009 May 18. [Epub ahead of print] To Reference
Ref 2Acute pancreatitis: animal models and recent advances in basic research. Pancreas. 2007 Jan;34(1):1-14. To Reference
Ref 3Enteropeptidase, a type II transmembrane serine protease. Front Biosci (Elite Ed). 2009 Jun 1;1:242-9. To Reference
Ref 4Identification and expression of the cDNA-encoding human mesotrypsin(ogen), an isoform of trypsin with inhibitor resistance. J Biol Chem. 1997 Apr 18;272(16):10573-8. To Reference
Ref 5Aprotinin decreases exposure to allogeneic blood during primary unilateral total hip replacement. J Bone Joint Surg Am. 2000 May;82(5):675-84. To Reference
Ref 6Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009 To Reference
Ref 7rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82. To Reference
Ref 8Optimization of the bioprocessing conditions for scale-up of transient production of a heterologous protein in plants using a chemically inducible viral amplicon expression system. Biotechnol Prog. 2009 May-Jun;25(3):722-34. To Reference
Ref 9Bioreactor strategies for improving production yield and functionality of a recombinant human protein in transgenic tobacco cell cultures. Biotechnol Bioeng. 2009 Feb 1;102(2):508-20. To Reference
Ref 10Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. To Reference
Ref 11J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. To Reference
Ref 12J 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 13J Med Chem. 1998 Mar 26;41(7):1060-7.2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease. To Reference
Ref 14Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. To Reference
Ref 15Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties. To Reference
Ref 16Bioorg. Med. Chem. Lett. 7(17):2205-2210 (1997) To Reference
Ref 17Overington 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 18Bioorg Med Chem Lett. 1999 Sep 6;9(17):2483-6.Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption. To Reference
Ref 19Bioorg Med Chem Lett. 2002 Apr 22;12(8):1203-8.Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. To Reference
Ref 20Bioorg Med Chem Lett. 1998 Nov 3;8(21):2955-60.5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor. To Reference
Ref 21J 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
Ref 22Bioorg Med Chem Lett. 1998 Dec 15;8(24):3603-8.Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety. To Reference
Ref 23Bioorg. Med. Chem. Lett. 7(1):67-72 (1997) To Reference
Ref 24Bioorg Med Chem Lett. 2003 Jan 20;13(2):161-4.Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'. To Reference
Ref 25Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6.Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. To Reference
Ref 26Bioorg Med Chem Lett. 2002 Mar 11;12(5):743-8.Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds. To Reference
Ref 27J Med Chem. 1995 Apr 28;38(9):1511-22.Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. To Reference
Ref 28J Med Chem. 2000 Aug 10;43(16):3033-44.GRID/CPCA: a new computational tool to design selective ligands. To Reference
Ref 29J Med Chem. 2005 Mar 24;48(6):1984-2008.In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design. To Reference
Ref 30J Med Chem. 2004 Feb 12;47(4):769-87.Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G. To Reference
Ref 31Bioorg Med Chem Lett. 2003 Feb 10;13(3):561-6.Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors. To Reference
Ref 32Bioorg Med Chem Lett. 1998 Aug 18;8(16):2235-40.Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors. To Reference
Ref 33Bioorg. Med. Chem. Lett. 6(24):2947-2952 (1996) To Reference
Ref 34J Med Chem. 1995 Oct 27;38(22):4446-53.Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions. To Reference



 

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