DGIdb - HEPARIN Drug Record

HEPARIN chembl:CHEMBL1909300

Alternate Names:

HEPARIN
HEPARINIC ACID
CALCIPARINE
HEPARIN SODIUM
HEP-LOCK
HEPARINATE
LIQUAEMIN
PANHEPRIN
SODIUM HEPARIN
chemidplus:9041-08-1
chembl:CHEMBL1909300
chemidplus:9005-49-6
drugbank:01109
pubchem.compound:22833565

Drug Info:

FDA Approval	not approved
Drug Indications	for treatment of cystic fibrosis
Drug Indications	for treatment of pelvic pain of bladder origin and interstitital cystitis
Drug Indications	antithrombotic
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	anticoagulant
Drug Class	anticoagulants
Year of Approval	approved before 1982

(2 More Sources)

Publications:

Chuang et al., 2001, Heparin enhances the specificity of antithrombin for thrombin and factor Xa independent of the reactive center loop sequence. Evidence for an exosite determinant of factor Xa specificity in heparin-activated antithrombin., J. Biol. Chem.
Schedin-Weiss et al., 2010, Kinetic evidence that allosteric activation of antithrombin by heparin is mediated by two sequential conformational changes., Arch. Biochem. Biophys.
Pappalardo et al., 2006, Anticoagulation management in patients undergoing open heart surgery by activated clotting time and whole blood heparin concentration., Perfusion
Sun et al., 2007, A fluorescent polymeric heparin sensor., Chemistry
Petitou et al., 1999, Synthesis of thrombin-inhibiting heparin mimetics without side effects., Nature
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Mirow et al., 2007, Plasma protein binding properties to immobilized heparin and heparin-albumin conjugate., Artif Organs
Gettins et al., 2009, Activation of antithrombin as a factor IXa and Xa inhibitor involves mitigation of repression rather than positive enhancement., FEBS Lett.
Sinosich et al., 1985, The influence of pergonal on in vitro production of placental protein 5 (PP5) by ovarian tumour cells., Tumour Biol.
Karnes JH et al., 2017, Influence of Human Leukocyte Antigen (HLA) Alleles and Killer Cell Immunoglobulin-Like Receptors (KIR) Types on Heparin-Induced Thrombocytopenia (HIT)., Pharmacotherapy
Berry et al., 2006, Heparin localization and fine structure regulate Burkitt's lymphoma growth., Biochem. Biophys. Res. Commun.
Nisoli et al., 2000, Induction of fatty acid translocase/CD36, peroxisome proliferator-activated receptor-gamma2, leptin, uncoupling proteins 2 and 3, and tumor necrosis factor-alpha gene expression in human subcutaneous fat by lipid infusion., Diabetes
Miyata et al., 1995, Interaction between casein kinase II and the 90-kDa stress protein, HSP90., Biochemistry
Patel et al., 2001, Chemokines have diverse abilities to form solid phase gradients., Clin. Immunol.
Randi et al., 1992, Recombinant von Willebrand factor Arg578-->Gln. A type IIB von Willebrand disease mutation affects binding to glycoprotein Ib but not to collagen or heparin., J. Biol. Chem.
Patey et al., 2006, Heparin derivatives as inhibitors of BACE-1, the Alzheimer's beta-secretase, with reduced activity against factor Xa and other proteases., J. Med. Chem.
Rezaie, 2000, Heparin-binding exosite of factor Xa., Trends Cardiovasc. Med.
Ignjatovic et al., 2007, Monitoring Unfractionated Heparin (UFH) therapy: which Anti-Factor Xa assay is appropriate?, Thromb. Res.
Rosenberg, 1985, Role of heparin and heparinlike molecules in thrombosis and atherosclerosis., Fed. Proc.
Van Iwaarden et al., 1994, Binding of surfactant protein A to the lipid A moiety of bacterial lipopolysaccharides., Biochem. J.
Fath et al., 1998, Interaction of secretory leukocyte protease inhibitor with heparin inhibits proteases involved in asthma., J. Biol. Chem.
Walter et al., 1996, Inhibition of human mast cell chymase by secretory leukocyte proteinase inhibitor: enhancement of the interaction by heparin., Arch. Biochem. Biophys.
Hansen et al., 2000, Reduction of factor FVIIa activity during heparin therapy. Evidence for assay interactions with tissue factor pathway inhibitor and antithrombin., Thromb. Res.
Whinna et al., 1993, Interaction of thrombin with antithrombin, heparin cofactor II, and protein C inhibitor., J. Protein Chem.
Park et al., 2001, Exploitation of syndecan-1 shedding by Pseudomonas aeruginosa enhances virulence., Nature
Harenberg et al., 1985, Anticoagulant and lipolytic effects of a low molecular weight heparin fraction., Thromb. Res.
Eckel et al., 1988, Plasma lipolytic activity. Relationship to postheparin lipolytic activity and evidence for metabolic regulation., Diabetes
Hallgren et al., 2004, Histidines are critical for heparin-dependent activation of mast cell tryptase., J. Immunol.
Bakillah et al., 1998, Lysine and arginine residues in the N-terminal 18% of apolipoprotein B are critical for its binding to microsomal triglyceride transfer protein., Biochemistry
Krul et al., 1988, Regional specificities of monoclonal anti-human apolipoprotein B antibodies., J. Lipid Res.
Hansen et al., 1995, Identification of a homologous heparin binding peptide sequence present in fibronectin and the 70 kDa family of heat-shock proteins., Biochim. Biophys. Acta
Wojtecka-Lukasik et al., 1984, Effects of neutral proteases from human leukocytes on plasma fibronectin., Thromb. Res.
Mathison et al., 2008, The tripeptide feG inhibits leukocyte adhesion., J Inflamm (Lond)
Bellosta et al., 2001, Identification of receptor and heparin binding sites in fibroblast growth factor 4 by structure-based mutagenesis., Mol. Cell. Biol.
Vettor et al., 2000, Substrate competition and insulin action in animal models., Int. J. Obes. Relat. Metab. Disord.
Gambetti et al., 2005, Interaction with heparin protects tissue transglutaminase against inactivation by heating and by proteolysis., Biochimie
Kolset et al., 1996, Serglycin-binding proteins in activated macrophages and platelets., J. Leukoc. Biol.
Okano et al., 2001, Biochemical characterization of cholesterol-3-sulfate as the sole effector for the phosphorylation of HMG1 by casein kinase I in vitro., Biochem. Biophys. Res. Commun.
Nakamura et al., 1995, Heparin-enhanced plasma phospholipase A2 activity and prostacyclin synthesis in patients undergoing cardiac surgery., J. Clin. Invest.

HEPARIN SLPI

Interaction Score: 6.6

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9593692 8615699

Sources:
NCI
HEPARIN SRGN

Interaction Score: 4.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8613703

Sources:
NCI
HEPARIN CCL21

Interaction Score: 4.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11286540

Sources:
NCI
HEPARIN TFPI2

Interaction Score: 4.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2416032

Sources:
NCI
HEPARIN TPSB2

Interaction Score: 2.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15265919

Sources:
NCI
HEPARIN SDC1

Interaction Score: 2.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11333985

Sources:
NCI
HEPARIN FGF4

Interaction Score: 1.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11486033

Sources:
NCI
HEPARIN HLA-DRB3

Interaction Score: 1.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28688202

Sources:
PharmGKB
HEPARIN SERPINA5

Interaction Score: 1.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8136018

Sources:
NCI
HEPARIN UCP2

Interaction Score: 1.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10868951

Sources:
NCI
HEPARIN SERPINC1

Interaction Score: 0.97

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name heparin

Novel drug target Established target

Trial Name heparin, oral, liquid

PMIDs:
11278930 20816747 17201083 17600786 10201371 11752352 17537059 19818773

Sources:
TdgClinicalTrial TEND GuideToPharmacology
HEPARIN LIPC

Interaction Score: 0.94

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
4082106 3360217

Sources:
NCI
HEPARIN PLA2G2A

Interaction Score: 0.63

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7883954

Sources:
NCI
HEPARIN F10

Interaction Score: 0.6

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name heparin

Novel drug target Established target

Trial Name heparin, oral, liquid

PMIDs:
17004727 11369259 17118432 3155697

Sources:
TdgClinicalTrial TEND
HEPARIN SFTPA1

Interaction Score: 0.55

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7980398

Sources:
NCI
HEPARIN NR5A1

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
6372156

Sources:
NCI
HEPARIN TFPI

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11150580

Sources:
NCI
HEPARIN APOB

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9521691 2457642

Sources:
NCI
HEPARIN VWF

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1400429

Sources:
NCI
HEPARIN CSNK1A1

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11243881

Sources:
NCI
HEPARIN FCGR3B

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18492254

Sources:
NCI
HEPARIN CSNK2A1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7794926

Sources:
NCI
HEPARIN TGM2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15935280

Sources:
NCI
HEPARIN FCGR3A

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18492254

Sources:
NCI
HEPARIN HPSE

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name M118

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
HEPARIN F2

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name octaparine, AVE-5026

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
HEPARIN HSPA4

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7548155

Sources:
NCI
HEPARIN SLC2A4

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10997602

Sources:
NCI
HEPARIN PIK3CG

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16904641

Sources:
NCI

TEND: HEPARIN
- Version: 01-August-2011
Alternate Names:

HEPARIN Primary Drug Name

Drug Info:

Year of Approval approved before 1982

Drug Class anticoagulants

Publications:
TdgClinicalTrial: HEPARIN
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications anticoagulant

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: HEPARIN

Version: 14-September-2017

Alternate Names:

C539 NCI drug code

Drug Info:

Publications:

Sinosich et al., 1985, The influence of pergonal on in vitro production of placental protein 5 (PP5) by ovarian tumour cells., Tumour Biol.

Park et al., 2001, Exploitation of syndecan-1 shedding by Pseudomonas aeruginosa enhances virulence., Nature

Bellosta et al., 2001, Identification of receptor and heparin binding sites in fibroblast growth factor 4 by structure-based mutagenesis., Mol. Cell. Biol.

PharmGKB: heparin
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Karnes JH et al., 2017, Influence of Human Leukocyte Antigen (HLA) Alleles and Killer Cell Immunoglobulin-Like Receptors (KIR) Types on Heparin-Induced Thrombocytopenia (HIT)., Pharmacotherapy
GuideToPharmacology: 178101031
- Version: 29-September-2020
Alternate Names:

HEPARIN GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1909300
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Trial Name	heparin
Novel drug target	Established target
Trial Name	heparin, oral, liquid

Trial Name	octaparine, AVE-5026
Novel drug target	Established target

activator (activating)
potentiator

HEPARIN Drug Record

HEPARIN chembl:CHEMBL1909300

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9593692 8615699

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8613703

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11286540

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2416032

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15265919

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11333985

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11486033

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28688202

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8136018

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10868951

Sources: NCI

Interaction Types & Directionality: activator (activating) potentiator

Interaction Info: Trial Name heparin Novel drug target Established target Trial Name heparin, oral, liquid

PMIDs: 11278930 20816747 17201083 17600786 10201371 11752352 17537059 19818773

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 4082106 3360217

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7883954

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name heparin Novel drug target Established target Trial Name heparin, oral, liquid

PMIDs: 17004727 11369259 17118432 3155697

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7980398

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 6372156

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11150580

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9521691 2457642

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1400429

Interaction Types & Directionality:

n/a

PMIDs:
9593692 8615699

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8613703

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11286540

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
2416032

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15265919

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11333985

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11486033

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
28688202

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
8136018

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
10868951

Sources:
NCI

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name heparin

Novel drug target Established target

Trial Name heparin, oral, liquid

PMIDs:
11278930 20816747 17201083 17600786 10201371 11752352 17537059 19818773

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
4082106 3360217

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
7883954

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name heparin

Novel drug target Established target

Trial Name heparin, oral, liquid

PMIDs:
17004727 11369259 17118432 3155697

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
7980398

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
6372156

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11150580

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
9521691 2457642

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
1400429

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
11243881

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18492254

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
7794926

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15935280

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18492254

Sources:
NCI

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name M118

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name octaparine, AVE-5026

Novel drug target Established target