General Information of Drug (ID: DM1PWX2)

Drug Name
Grassystatin a Drug Info
Synonyms Grassystatin A; CHEMBL567893; GTPL8674
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
44255320
TTD Drug ID
DM1PWX2

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pentamidine DMHZJCG African trypanosomiasis 1F51 Approved [3]
Lactoferrin DMA7QTC Solid tumour/cancer 2A00-2F9Z Approved [3]
APC-2059 DM8IB6K Inflammatory bowel disease DD72 Discontinued in Phase 2 [4]
APC-366 DM02DNQ Asthma CA23 Discontinued in Phase 2 [3]
BABIM DM8AGOE Asthma CA23 Terminated [3]
BAY-17-1998 DM7LZFQ Asthma CA23 Terminated [5]
BAY-44-3428 DM40ORU Asthma CA23 Terminated [6]
BMS-262084 DMETNA3 Discovery agent N.A. Investigative [7]
AMG-126737 DM9H7AZ Discovery agent N.A. Investigative [8]
MOL 6131 DMSF8UC Discovery agent N.A. Investigative [8]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Alpha 1-PI DMXC1K9 Alpha-1 antitrypsin deficiency 5C5A Approved [9]
Erdosteine DM6QFSV Bronchitis CA20 Approved [10]
Sivelestat DM6BZCV Crohn disease DD70 Phase 3 [11]
Mdl 101,146 DMRSOBG Inflammation 1A00-CA43.1 Terminated [12]
WIN-63759 DMRV48P Emphysema CA21 Terminated [13]
SSR-69071 DMWL4MI Chronic obstructive pulmonary disease CA22 Terminated [14]
SYN-1134 DMG2SQM Cystic fibrosis CA25 Terminated [15]
PBI-1101 DMWD1RC Inflammation 1A00-CA43.1 Terminated [16]
Acetate Ion DMD08RH Discovery agent N.A. Investigative [12]
Dimethylformamide DML6O4N Discovery agent N.A. Investigative [17]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bortezomib DMNO38U Leukemia Approved [18]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [19]
Ulinastatin DMIQCFG Premature labour JB00 Phase 3 [20]
Alpha-1 antitrypsin DM5EFXZ Coagulation defect 3B10.0 Phase 2 [21]
Dermolastin DM6WSU2 Atopic dermatitis EA80 Discontinued in Phase 2 [22]
RWJ-56423 DM6BIHE Asthma CA23 Discontinued in Phase 1 [23]
Patamostat DM6HBQJ Hypotension BA20-BA21 Terminated [21]
BMY-44621 DM8R3N0 N. A. N. A. Terminated [24]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine DM3UMYD Discovery agent N.A. Investigative [25]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine DME3PUT Discovery agent N.A. Investigative [26]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Cathepsin D (CTSD)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID10498202C1 DMXE0F2 Multiple sclerosis 8A40 Clinical trial [27]
CI-992 DMBHYIJ Hypertension BA00-BA04 Terminated [28]
Alpha-D-Mannose DMF5DLW Discovery agent N.A. Investigative [12]
PMID8410973C3 DM6J5KY Discovery agent N.A. Investigative [29]
KNI-10006 DMMISH6 Discovery agent N.A. Investigative [30]
GRL-7234 DMR93MK Discovery agent N.A. Investigative [31]
S-Methylcysteine DMAMRKS Discovery agent N.A. Investigative [12]
Carbocyclic Peptidomimetic DM87SOX Discovery agent N.A. Investigative [32]
N-Aminoethylmorpholine DMWXBYC Discovery agent N.A. Investigative [12]
1h-Benoximidazole-2-Carboxylic Acid DMNZAVE Discovery agent N.A. Investigative [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Plasminogen (PLG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ranolazine DM0C9IL Acute coronary syndrome BA41 Approved [33]
Aminocaproic Acid DMFGND4 Bleeding disorder GA20-GA21 Approved [34]
Streptokinase DM5JQ0D Pulmonary embolism BB00 Approved [35]
Tranexamic Acid DMFI8A7 Excessive bleeding GA30.02 Approved [36]
Alteplase DMRJ3YX Acute myocardial infarction BA41 Approved [37]
Tenecteplase DMJYN25 Acute myocardial infarction BA41 Approved [37]
Anistreplase DM6Q4B0 Acute coronary syndrome BA41 Approved [38]
Reteplase DML0D1P Heart attack BA41 Approved [39]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [19]
Desmoteplase DMDLU4Z Ischemic stroke 8B11.5Z Phase 3 [40]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Caspase-11 (CASP11) TT6KIOT CASP4_HUMAN Inhibitor [2]
Cathepsin D (CTSD) TTPT2QI CATD_HUMAN Inhibitor [2]
Cationic trypsinogen (PRSS1) TT2WR1T TRY1_HUMAN Inhibitor [2]
Pancreatic elastase 1 (CELA1) TT3NKIB CELA1_HUMAN Inhibitor [2]
Plasminogen (PLG) TTP86E2 PLMN_HUMAN Inhibitor [2]
Tryptase alpha/beta-1 (Tryptase) TTM1TDX TRYB1_HUMAN Inhibitor [2]

References

1 URL: 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: 8674).
2 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.
3 Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96.
4 Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002 Mar;16(3):407-13.
5 Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire
6 Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire
7 Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.
8 Tryptase inhibition blocks airway inflammation in a mouse asthma model. J Immunol. 2002 Feb 15;168(4):1992-2000.
9 Elastase inhibitors. J Soc Biol. 2001;195(2):143-50.
10 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
11 Sivelestat (selective neutrophil elastase inhibitor) improves the mortality rate of sepsis associated with both acute respiratory distress syndrome... Shock. 2010 Jan;33(1):14-8.
12 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
13 Biological activity of WIN 63759, an orally bioavailable inhibitor of human neutrophil elastase. Drug Development Research Volume 34, Issue 3, pages 306-316, March 1995.
14 Pivotal role for alpha1-antichymotrypsin in skin repair. J Biol Chem. 2011 Aug 19;286(33):28889-901.
15 EP patent application no. 1292314, Method for treating respiratory disorders associated with pulmonary elastic fiber injury comprising the use of glycosaminoglycans.
16 CN patent application no. 1813706, Use of elastic protease inhibitor for preparing medicine for protecting cerebral hemorrhage.
17 Liver disease associated with occupational exposure to the solvent dimethylformamide. Ann Intern Med. 1988 May;108(5):680-6.
18 Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. J Med Chem. 1995 Apr 28;38(9):1511-22.
19 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
20 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.
21 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.
22 Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
23 Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G. J Med Chem. 2004 Feb 12;47(4):769-87.
24 Design and synthesis of conformationally constrained arginal thrombin inhibitors, Bioorg. Med. Chem. Lett. 7(17):2205-2210 (1997).
25 Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasmi... J Med Chem. 2001 Aug 16;44(17):2753-71.
26 Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.
27 Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2531-6.
28 Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors. J Med Chem. 1992 Jul 10;35(14):2562-72.
29 Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation. J Med Chem. 1993 Sep 3;36(18):2614-20.
30 alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases. Bioorg Med Chem. 2009 Aug 15;17(16):5933-49.
31 Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands. J Med Chem. 2007 May 17;50(10):2399-407.
32 Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics. J Med Chem. 2005 Aug 11;48(16):5175-90.
33 Tranexamic acid in trauma: how should we use it. J Trauma Acute Care Surg. 2013 Jun;74(6):1575-86.
34 The blockage of the high-affinity lysine binding sites of plasminogen by EACA significantly inhibits prourokinase-induced plasminogen activation. Biochim Biophys Acta. 2002 Apr 29;1596(2):182-92.
35 Acute anuric renal failure with streptokinase therapy in a patient with acute venous thromboembolic disease and the review of renal side effects of streptokinase. Tuberk Toraks. 2008;56(4):456-61.
36 Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8.
37 Thrombolytic therapies: the current state of affairs. J Endovasc Ther. 2005 Apr;12(2):224-32.
38 Evaluation of thrombolytic agents. Drugs. 1997;54 Suppl 3:11-6; discussion 16-7.
39 Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.
40 Vampire bat salivary plasminogen activator (desmoteplase): a unique fibrinolytic enzyme that does not promote neurodegeneration. Stroke. 2003 Feb;34(2):537-43.