Target Information

Target General Infomation
Target ID
T73476
Former ID
TTDS00467
Target Name
Antithrombin-III
Gene Name
SERPINC1
Synonyms
AT3; ATIII; SERPINC1
Target Type
Successful
Disease Acute coronary syndrome [ICD9: 444; ICD10: I74]
Asthma [ICD10: J45]
Blood coagulation disorders [ICD10: D65-D68]
Central or sensorineural tinnitus [ICD9: 388.3; ICD10: H93.1]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Coagulation [ICD10: I80-I82]
Deep vein thrombosis [ICD9: 437.6, 453, 453.40, 671.5, 671.9; ICD10: I80-I82, I80.2]
Phlebothrombosis [ICD10: I80-I82]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Ulcerative colitis [ICD9: 556; ICD10: K51]
Venous thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Unspecified [ICD code not available]
Function
Most important serine protease inhibitorin plasma that regulates the blood coagulation cascade. At-iii inhibits thrombin as well as factors ixa, xa and xia. Its inhibitory activity is greatly enhanced in the presence of heparin.
BioChemical Class
Serpin family
UniProt ID
P01008
Sequence
MYSNVIGTVTSGKRKVYLLSLLLIGFWDCVTCHGSPVDICTAKPRDIPMNPMCIYRSPEK
KATEDEGSEQKIPEATNRRVWELSKANSRFATTFYQHLADSKNDNDNIFLSPLSISTAFA
MTKLGACNDTLQQLMEVFKFDTISEKTSDQIHFFFAKLNCRLYRKANKSSKLVSANRLFG
DKSLTFNETYQDISELVYGAKLQPLDFKENAEQSRAAINKWVSNKTEGRITDVIPSEAIN
ELTVLVLVNTIYFKGLWKSKFSPENTRKELFYKADGESCSASMMYQEGKFRYRRVAEGTQ
VLELPFKGDDITMVLILPKPEKSLAKVEKELTPEVLQEWLDELEEMMLVVHMPRFRIEDG
FSLKEQLQDMGLVDLFSPEKSKLPGIVAEGRDDLYVSDAFHKAFLEVNEEGSEAAASTAV
VIAGRSLNPNRVTFKANRPFLVFIREVPLNTIIFMGRVANPCVK
Drugs and Mode of Action
Drug(s) Ardeparin Drug Info Approved Deep vein thrombosis [1]
Enoxaparin Drug Info Approved Venous thrombosis [1], [2]
Heparin Drug Info Approved Deep vein thrombosis [3]
Heparin Calcium Drug Info Approved Coagulation [4]
Heparin Sodium Drug Info Approved Coagulation [4]
Sulodexide Drug Info Approved Central or sensorineural tinnitus [5]
Heparin low molecular weight Drug Info Phase 3 Thrombosis [6]
KW-3357 Drug Info Phase 3 Blood coagulation disorders [7]
Low molecular weight heparin Drug Info Phase 3 Thrombosis [8]
Unfractionated heparin Drug Info Phase 3 Thrombosis [9]
M118 Drug Info Phase 2 Acute coronary syndrome [10]
O-desulfated heparin Drug Info Phase 2 Chronic obstructive pulmonary disease [11]
PMX-60056 Drug Info Phase 2 Blood coagulation disorders [12]
MER-102 Drug Info Phase 1 Thrombosis [13]
OPK-0018 Drug Info Phase 1 Asthma [14]
RO-14 Drug Info Phase 1 Phlebothrombosis [15]
Unfractionated heparin Drug Info Phase 1 Thrombosis [16]
Deligoparin sodium Drug Info Discontinued in Phase 3 Ulcerative colitis [17]
Inhibitor Alpha-D-Mannose Drug Info [18]
Heparin Pentasaccharide Drug Info [18]
M118 Drug Info [19]
MER-102 Drug Info [20]
N-Formylmethionine Drug Info [18]
Modulator antithrombin III, Aventis Behring Drug Info
Ardeparin Drug Info [21]
Deligoparin sodium Drug Info [22]
Enoxaparin Drug Info [21]
Heparin Drug Info [22]
Heparin Calcium Drug Info [21]
Heparin low molecular weight Drug Info [23]
Heparin Sodium Drug Info [21]
KW-3357 Drug Info
LHD-4 Drug Info [22]
Low molecular weight heparin Drug Info [24]
Non-anticoagulation heparins Drug Info [22]
O-desulfated heparin Drug Info [25]
Org-36764 Drug Info
PNU-87663 Drug Info
RO-14 Drug Info [26]
Unfractionated heparin Drug Info [27]
Antagonist OPK-0018 Drug Info [22]
PMX-60056 Drug Info [28]
Activator Sulodexide Drug Info [29], [30]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Complement and coagulation cascades
PANTHER Pathway Blood coagulation
Pathway Interaction Database Glypican 1 network
Reactome Intrinsic Pathway of Fibrin Clot Formation
Common Pathway of Fibrin Clot Formation
WikiPathways Complement and Coagulation Cascades
Formation of Fibrin Clot (Clotting Cascade)
References
REF 1Pharmacologic profile of certoparin. Expert Opin Investig Drugs. 1999 Mar;8(3):315-27.
REF 2(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: 6811).
REF 3(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: 4214).
REF 4Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 5Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
REF 6Low-molecular-weight heparin in patients with advanced cancer: a phase 3 clinical trial. Mayo Clin Proc. 2006 Jun;81(6):758-67.
REF 7ClinicalTrials.gov (NCT01384903) An Open-label Study of KW-3357. U.S. National Institutes of Health.
REF 8Clinical pipeline report, company report or official report of Emisphere Technologies Inc.
REF 9Bivalirudin as a replacement for unfractionated heparin in unstable angina/non-ST-elevation myocardial infarction: observations from the TIMI 8 trial. The Thrombolysis in Myocardial Infarction. Am Heart J. 2002 Feb;143(2):229-34.
REF 10Clinical pipeline report, company report or official report of Momenta Pharmaceuticals.
REF 11ClinicalTrials.gov (NCT01461915) Efficacy & Safety of ODSH (2-0, 3-0 Desulfated Heparin) in Patients With Metastatic Pancreatic Cancer Treated With Gemcitabine & Abraxane. U.S. National Institutes ofHealth.
REF 12ClinicalTrials.gov (NCT01312935) Reversal of Heparin in Patients Undergoing Percutaneous Coronary Intervention (PCI). U.S. National Institutes of Health.
REF 13Fondaparinux sodium. Drugs Today (Barc). 2002 Mar;38(3):185-94.
REF 14Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034071)
REF 15ClinicalTrials.gov (NCT00629733) Clinical Trial to Evaluate the Tolerability and Pharmacokinetics of a New Ultra Low Molecular Weight Heparin (RO-14) Administered Subcutaneously Increasing Single-doses to Healthy Male Volunteers. U.S. National Institutes of Health.
REF 16Clinical pipeline report, company report or official report of Emisphere Technologies.
REF 17Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006120)
REF 18How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 19Clinical pipeline report, company report or official report of Momentapharma.
REF 20Clinical pipeline report, company report or official report of Merrion's GIPET technology.
REF 21Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 22(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. (Target id: 2632).
REF 23Effects of low molecular weight heparin on a severely antithrombin III-decreased disseminated intravascular coagulation model in rabbits. Thromb Res. 1995 Dec 1;80(5):391-8.
REF 24Oral heparin: status review. Thromb J. 2006; 4: 6.
REF 25Structural determinants of the capacity of heparin to inhibit the formation of the human amplification C3 convertase. J Clin Invest. 1981 Jan;67(1):223-8.
REF 26Pharmacological effects and clinical applications of ultra low molecular weight heparins. Drug Discov Ther. 2014 Feb;8(1):1-10.
REF 27Heparin with low affinity to antithrombin III inhibits the activation of prothrombin in normal plasma. Thromb Res. 1982 Nov 15;28(4):487-97.
REF 28Parenteral Anticoagulants: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines. Correction in: Chest. 2013 August; 144(2): 721.
REF 29Management of tinnitus: oral treatment with melatonin and sulodexide. J Biol Regul Homeost Agents. 2009 Apr-Jun;23(2):103-10.
REF 30Review of pharmacodynamics, pharmacokinetics, and therapeutic properties of sulodexide. Med Res Rev. 1998 Jan;18(1):1-20.

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