DGIdb - SERPINC1 Gene Record

SERPINC1 462 Druggable Genome

Alternate Names:

462
SERPIN FAMILY C MEMBER 1
SERPINC1
AT3
AT3D
ATIII
THPH7
107300
775
ENSG00000117601
OTTHUMG00000037276
P01008
ANT3_HUMAN
ANTITHROMBIN-III
Serpin C1
ANTITHROMBIN-III PRECURSOR (ATIII). [SOURCE:UNIPROT/SWISSPROT;ACC:P01008]
PA35026
T73476
ATIII-R2
ATIII-T1
ATIII-T2

Gene Info:

Target Main Class	Other
Target Subclass	Enzyme Inhibitor
Human Readable Name	PROTEASE INHIBITOR
Human Readable Name	DRUGGABLE GENOME
Interpro Short Name	Serpin_fam
Interpro Acc	IPR000215
Interpro Type	Family
Interpro Name	Serpin family
Uniprot Evidence	1: Evidence at protein level
Uniprot Status	Swiss-Prot
Target Class	Miscellaneous
Target Subclass	Enzyme regulator
Target Class	Other
Gene Biotype	PROTEIN_CODING

(7 More Sources)

Gene Categories: Category Details

PROTEASE INHIBITOR
DRUGGABLE GENOME

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.
Cosmi et al., 2003, Additive thrombin inhibition by fast moving heparin and dermatan sulfate explains the anticoagulant effect of sulodexide, a natural mixture of glycosaminoglycans., Thromb. Res.
Harenberg, 1998, Review of pharmacodynamics, pharmacokinetics, and therapeutic properties of sulodexide., Med Res Rev
Donat et al., 2002, The pharmacokinetics of fondaparinux sodium in healthy volunteers., Clin Pharmacokinet
Cheng, 2002, Fondaparinux: a new antithrombotic agent., Clin Ther
Dager et al., 2004, Special considerations with fondaparinux therapy: heparin-induced thrombocytopenia and wound healing., Pharmacotherapy
Paolucci et al., 2002, Fondaparinux sodium mechanism of action: identification of specific binding to purified and human plasma-derived proteins., Clin Pharmacokinet
Arbit E et al., 2006, Oral heparin: status review., Thromb J
Bisio et al., 2009, Structural features of low-molecular-weight heparins affecting their affinity to antithrombin., Thromb. Haemost.
Peng et al., 2005, [Effects of thrombolysis and anticoagulation on the functions of vascular endothelial cells and coagulation and fibrinolysis in patients with pulmonary thromboembolism]., Zhonghua Jie He He Hu Xi Za Zhi
Lee et al., 2007, Enoxaparin in acute coronary syndromes., Expert Rev Cardiovasc Ther
Florian-Kujawski et al., 2004, Differential regulation of thrombin activatable fibrinolytic inhibitor by low molecular weight heparins. Pharmacologic implications., Int Angiol
Morris et al., 2005, Pharmacokinetics of UH and LMWH are similar with respect to antithrombin activity., Thromb. Res.
Björn N et al., 2020, Genes and variants in hematopoiesis-related pathways are associated with gemcitabine/carboplatin-induced thrombocytopenia., Pharmacogenomics J
Garcia DA et al., 2012, Parenteral anticoagulants: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines., Chest
Lin et al., 2001, Antithrombin binding of low molecular weight heparins and inhibition of factor Xa., Biochim. Biophys. Acta
Shaughnessy et al., 1995, The effects of low molecular weight and standard heparin on calcium loss from fetal rat calvaria., Blood
Mousa, 2002, The low molecular weight heparin, tinzaparin, in thrombosis and beyond., Cardiovasc Drug Rev

FONDAPARINUX SERPINC1

Interaction Score: 16.13

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12383039 12501872 15317404 12383040

Sources:
TdgClinicalTrial TEND
ARDEPARIN SODIUM SERPINC1

Interaction Score: 10.75

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
11287128 7632944 12397367

Sources:
ChemblInteractions
SULODEXIDE SERPINC1

Interaction Score: 8.06

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name sulodexide, KRX-101,Sulonex

PMIDs:
12818259 11752352 9436179

Sources:
TdgClinicalTrial TEND TTD
DELPARANTAG SERPINC1

Interaction Score: 5.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22315264

Sources:
TTD
TINZAPARIN SERPINC1

Interaction Score: 5.38

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name tinzaparin sodium injection,Innohep

Novel drug target Established target

PMIDs:
15767980 15567452 19888521

Sources:
TdgClinicalTrial
ENOXAPARIN SERPINC1

Interaction Score: 5.38

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

PMIDs:
16686945 19888521 16207425 17489664

Sources:
TEND TTD
SEMULOPARIN SODIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Antithrombin-III inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ANTITHROMBIN ALFA SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
HEPARIN SODIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HEPARIN CALCIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DANAPAROID SODIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DALTEPARIN SODIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Antithrombin-III activator

PMIDs:
None found

Sources:
ChemblInteractions
FONDAPARINUX SODIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TINZAPARIN SODIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Antithrombin-III activator

PMIDs:
None found

Sources:
ChemblInteractions
ENOXAPARIN SODIUM SERPINC1

Interaction Score: 2.69

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HEPARIN SERPINC1

Interaction Score: 0.93

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
LUSUTROMBOPAG SERPINC1

Interaction Score: 0.9

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
ELTROMBOPAG SERPINC1

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
AVATROMBOPAG SERPINC1

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
ESTRADIOL SERPINC1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Estradiol,Progesterone

PMIDs:
None found

Sources:
FDA
CARBOPLATIN SERPINC1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31616045

Sources:
PharmGKB
GEMCITABINE SERPINC1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31616045

Sources:
PharmGKB
PROGESTERONE SERPINC1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Estradiol,Progesterone

PMIDs:
None found

Sources:
FDA

Ensembl: ENSG00000117601
- Version: 101_38
Alternate Names:

SERPINC1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P01008
- Version: 01-August-2011
Alternate Names:

462 Entrez Gene Id

SERPINC1 Gene Symbol

ANT3_HUMAN Uniprot Id

Gene Info:

Target Main Class Other

Target Subclass Enzyme Inhibitor

Publications:
RussLampel: ENSG00000117601
- Version: 26-July-2011
Alternate Names:

ENSG00000117601 Ensembl Gene Id

ANTITHROMBIN-III PRECURSOR (ATIII). [SOURCE:UNIPROT/SWISSPROT;ACC:P01008] Description

SERPINC1 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P01008
- Version: January-2014
Alternate Names:

SERPINC1 Gene Symbol

Gene Info:

Target Class Miscellaneous

Target Subclass Enzyme regulator

Target Class Other

Publications:
HopkinsGroom: P01008
- Version: 11-September-2012
Alternate Names:

SERPINC1 Uniprot Gene Name

P01008 Uniprot Accession

462 Entrez Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Interpro Short Name Serpin_fam

Interpro Acc IPR000215

Gene Categories:

PROTEASE INHIBITOR, DRUGGABLE GENOME

Publications:
PharmGKB: SERPINC1
- Version: 18-August-2020
Alternate Names:

PA35026 PharmGKB ID

Gene Info:

Publications:

Björn N et al., 2020, Genes and variants in hematopoiesis-related pathways are associated with gemcitabine/carboplatin-induced thrombocytopenia., Pharmacogenomics J

TTD: Antithrombin-III

Version: 2020.06.01

Alternate Names:

ATIII TTD Gene Abbreviation

T73476 TTD Target ID

Gene Info:

Publications:

Garcia DA et al., 2012, Parenteral anticoagulants: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines., Chest

Arbit E et al., 2006, Oral heparin: status review., Thromb J

HingoraniCasas: ENSG00000117601
- Version: 31-May-2017
Alternate Names:

ENSG00000117601 Gene Symbol

SERPINC1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: AT3
- Version: chembl_23
Alternate Names:

AT3 GENE_SYMBOL

SERPINC1 GENE_SYMBOL

Antithrombin-III UNIPROT

Gene Info:

Publications:
dGene: SERPINC1
- Version: 27-Jun-2013
Alternate Names:

462 Gene ID

AT3 dGene Synonym

AT3D dGene Synonym

Gene Info:

Gene Categories:

PROTEASE INHIBITOR

Publications:
FDA: SERPINC1
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:

Mechanism of Interaction	Antithrombin-III activator
Direct Interaction	yes

Novel drug target	Established target
Trial Name	sulodexide, KRX-101,Sulonex

Trial Name	tinzaparin sodium injection,Innohep
Novel drug target	Established target

Mechanism of Interaction	Antithrombin-III inhibitor
Direct Interaction	yes

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

ENSG00000117601	Ensembl Gene Id
ANTITHROMBIN-III PRECURSOR (ATIII). [SOURCE:UNIPROT/SWISSPROT;ACC:P01008]	Description
SERPINC1	Display Id

SERPINC1	Uniprot Gene Name
P01008	Uniprot Accession
462	Entrez Gene Id

activator (activating)
potentiator

activator (activating)
potentiator

activator (activating)
potentiator

activator (activating)
potentiator

SERPINC1 Gene Record

SERPINC1 462 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: activator (activating) potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12383039 12501872 15317404 12383040

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: activator (activating) potentiator

Interaction Info: Mechanism of Interaction Antithrombin-III activator Direct Interaction yes

PMIDs: 11287128 7632944 12397367

Sources: ChemblInteractions

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name sulodexide, KRX-101,Sulonex

PMIDs: 12818259 11752352 9436179

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22315264

Sources: TTD

Interaction Types & Directionality: activator (activating) potentiator

Interaction Info: Trial Name tinzaparin sodium injection,Innohep Novel drug target Established target

PMIDs: 15767980 15567452 19888521

Sources: TdgClinicalTrial

Interaction Types & Directionality: activator (activating) potentiator

Interaction Info:

PMIDs: 16686945 19888521 16207425 17489664

Sources: TEND TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Antithrombin-III inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: activator (activating)

Interaction Info: Mechanism of Interaction Antithrombin-III activator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Mechanism of Interaction Antithrombin-III activator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Mechanism of Interaction Antithrombin-III activator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Antithrombin-III activator

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Mechanism of Interaction Antithrombin-III activator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Antithrombin-III activator

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Mechanism of Interaction Antithrombin-III activator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12383039 12501872 15317404 12383040

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
11287128 7632944 12397367

Sources:
ChemblInteractions

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name sulodexide, KRX-101,Sulonex

PMIDs:
12818259 11752352 9436179

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
22315264

Sources:
TTD

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name tinzaparin sodium injection,Innohep

Novel drug target Established target

PMIDs:
15767980 15567452 19888521

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

activator (activating)

potentiator

PMIDs:
16686945 19888521 16207425 17489664

Sources:
TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Antithrombin-III inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Antithrombin-III activator

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Antithrombin-III activator

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Antithrombin-III activator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

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

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

Combination therapy Estradiol,Progesterone

PMIDs:
None found

Sources:
FDA

Interaction Types & Directionality:

n/a

PMIDs:
31616045

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
31616045

Sources:
PharmGKB