Target Information
Target General Infomation | |||||
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Target ID |
T27602
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Former ID |
TTDS00282
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Target Name |
Trypsin
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Gene Name |
PRSS1
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Synonyms |
Trypsinogen; PRSS1
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Target Type |
Clinical Trial
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Disease | Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99] | ||||
Asthma [ICD10: J45] | |||||
Blood coagulation disorders [ICD10: D65-D68] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Hypotension [ICD9: 458, 796.3; ICD10: I95] | |||||
Premature labour [ICD9: 644, 765; ICD10: O60.1, P07.3] | |||||
Unspecified [ICD code not available] | |||||
BioChemical Class |
Peptidase
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Target Validation |
T27602
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UniProt ID | |||||
EC Number |
EC 3.4.21.4
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Sequence |
MNPLLILTFVAAALAAPFDDDDKIVGGYNCEENSVPYQVSLNSGYHFCGGSLINEQWVVS
AGHCYKSRIQVRLGEHNIEVLEGNEQFINAAKIIRHPQYDRKTLNNDIMLIKLSSRAVIN ARVSTISLPTAPPATGTKCLISGWGNTASSGADYPDELQCLDAPVLSQAKCEASYPGKIT SNMFCVGFLEGGKDSCQGDSGGPVVCNGQLQGVVSWGDGCAQKNKPGVYTKVYNYVKWIK NTIAANS |
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Drugs and Mode of Action | |||||
Drug(s) | MELAGATRAN | Drug Info | Phase 3 | Discovery agent | [521709], [541520] |
Ulinastatin | Drug Info | Phase 3 | Premature labour | [532738] | |
Alpha-1 antitrypsin | Drug Info | Phase 2 | Blood coagulation disorders | [526002] | |
Dermolastin | Drug Info | Discontinued in Phase 2 | Atopic dermatitis | [547642] | |
RWJ-56423 | Drug Info | Discontinued in Phase 1 | Asthma | [526697] | |
BMY-44621 | Drug Info | Terminated | Discovery agent | [545449] | |
Patamostat | Drug Info | Terminated | Hypotension | [545400] | |
Inhibitor | 1,3-Di-p-tolyl-[1,3]diazetidine-2,4-dione | Drug Info | [526092] | ||
1,3-Dibenzyl-[1,3]diazetidine-2,4-dione | Drug Info | [526092] | |||
1-(3-Amino-benzyl)-1H-indole-5-carboxamidine | Drug Info | [533527] | |||
1-(3-Nitro-benzyl)-1H-indole-5-carboxamidine | Drug Info | [533527] | |||
1-Benzyl-1H-indole-5-carboxamidine | Drug Info | [533527] | |||
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine | Drug Info | [526118] | |||
2-(2-Iodo-phenyl)-benzo[d][1,3]oxazin-4-one | Drug Info | [534598] | |||
2-Propionyl-1H-indole-6-carboxamidine | Drug Info | [533527] | |||
4-(3,4-Diethoxy-benzylamino)-benzamidine | Drug Info | [527397] | |||
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine | Drug Info | [527397] | |||
4-(5-Nitro-indol-1-ylmethyl)-benzamidine | Drug Info | [533527] | |||
4-Indol-1-ylmethyl-benzamidine | Drug Info | [533527] | |||
6-Styryl-naphthalene-2-carboxamidine | Drug Info | [527320] | |||
8-Bromo-6-styryl-naphthalene-2-carboxamidine | Drug Info | [527320] | |||
8-Furan-3-yl-6-styryl-naphthalene-2-carboxamidine | Drug Info | [527320] | |||
Benzamidine | Drug Info | [551393] | |||
Benzamidrazone analogue | Drug Info | [525596] | |||
BMY-44621 | Drug Info | [551325] | |||
compound 9 | Drug Info | [533458] | |||
CVS-2139 | Drug Info | [526306] | |||
CVS-2359 | Drug Info | [526306] | |||
Dermolastin | Drug Info | [536190], [536840], [537435], [551533] | |||
GR-133686 | Drug Info | [534803] | |||
GRASSYSTATIN A | Drug Info | [530345] | |||
L-375378 | Drug Info | [526487] | |||
Macrocyclic tripeptide motif | Drug Info | [551309] | |||
MELAGATRAN | Drug Info | [528066] | |||
P1 argininal derivative | Drug Info | [526275] | |||
Peptide boronate | Drug Info | [533716] | |||
Piperidine-1-carboxamidine | Drug Info | [525858] | |||
RWJ-50353 | Drug Info | [527480] | |||
RWJ-56423 | Drug Info | [526956] | |||
Tert-butyloxy carbonyl-D-Phe-pro-Arg-H | Drug Info | [533588] | |||
Modulator | Alpha-1 antitrypsin | Drug Info | [526791], [549592], [550162] | ||
ATF-HI-8 | Drug Info | ||||
JBP-1 | Drug Info | [549592], [550162] | |||
Patamostat | Drug Info | [533452], [549592], [550162] | |||
POP-1 | Drug Info | [549592], [550162] | |||
recAAT, PPL Therapeutics/Bayer | Drug Info | ||||
Ulinastatin | Drug Info | [532738] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
DRM | DRM Info | ||||
Pathways | |||||
References | |||||
Ref 521709 | ClinicalTrials.gov (NCT00206089) Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events. U.S. National Institutes of Health. | ||||
Ref 526002 | Technology evaluation: transgenic alpha-1-antitrypsin (AAT), PPL therapeutics. Curr Opin Mol Ther. 2000 Apr;2(2):199-204. | ||||
Ref 526697 | Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone. J Med Chem. 2003 Aug 28;46(18):3865-76. | ||||
Ref 532738 | Intravenous administration of ulinastatin (human urinary trypsin inhibitor) in severe sepsis: a multicenter randomized controlled study. Intensive Care Med. 2014 Jun;40(6):830-8. | ||||
Ref 541520 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6382). | ||||
Ref 545400 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003114) | ||||
Ref 525596 | Bioorg Med Chem Lett. 1999 Sep 6;9(17):2483-6.Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption. | ||||
Ref 525858 | J Med Chem. 2000 Aug 10;43(16):3033-44.GRID/CPCA: a new computational tool to design selective ligands. | ||||
Ref 526092 | Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. | ||||
Ref 526118 | J 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. | ||||
Ref 526275 | Bioorg Med Chem Lett. 2002 Mar 11;12(5):743-8.Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds. | ||||
Ref 526306 | Bioorg Med Chem Lett. 2002 Apr 22;12(8):1203-8.Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. | ||||
Ref 526487 | Bioorg 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'. | ||||
Ref 526791 | Expression of human alpha 1 antitrypsin in transgenic sheep. Cytotechnology. 1992;9(1-3):77-84. | ||||
Ref 526956 | J 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. | ||||
Ref 527320 | Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties. | ||||
Ref 527397 | Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. | ||||
Ref 527480 | J 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. | ||||
Ref 528066 | Bioorg 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. | ||||
Ref 530345 | J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. | ||||
Ref 532738 | Intravenous administration of ulinastatin (human urinary trypsin inhibitor) in severe sepsis: a multicenter randomized controlled study. Intensive Care Med. 2014 Jun;40(6):830-8. | ||||
Ref 533452 | Effects of E-3123, a new protease inhibitor, on several protease activities and on experimental acute pancreatitis. Nihon Yakurigaku Zasshi. 1988 May;91(5):285-93. | ||||
Ref 533458 | Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates. J Med Chem. 1986 Apr;29(4):514-9. | ||||
Ref 533527 | J 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. | ||||
Ref 533588 | J 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. | ||||
Ref 533716 | J 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. | ||||
Ref 534598 | J Med Chem. 1998 Mar 26;41(7):1060-7.2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease. | ||||
Ref 534803 | Bioorg 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. | ||||
Ref 536840 | Bioreactor 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. | ||||
Ref 537435 | Optimization 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. | ||||
Ref 549592 | US patent application no. 2012,0251,516, PHARMACEUTICAL COMPOSITION FOR TREATING CANCER COMPRISING TRYPSINOGEN AND/OR CHYMOTRYPSINOGEN AND AN ACTIVE AGENT SELECTED FROM A SELENIUM COMPOUND, A VANILLOID COMPOUND AND A CYTOPLASMIC GLYCOLYSIS REDUCTION AGENT. | ||||
Ref 550162 | EP patent application no. 2490711, A pharmaceutical composition for treating cancer comprising trypsinogen and/or chymotrypsinogen and an active agent selected from a selenium compound, a vanilloid compound and a cytoplasmic glycolysis reduction agent). | ||||
Ref 551309 | Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif, Bioorg. Med. Chem. Lett. 6(24):2947-2952 (1996). |
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