DGIdb - F2 Gene Record

F2 2147 Druggable Genome

Alternate Names:

2147
COAGULATION FACTOR II, THROMBIN
F2
PT
RPRGL2
THPH1
176930
3535
ENSG00000180210
OTTHUMG00000150344
Activation peptide fragment 1
Prothrombin
Activation peptide fragment 2
Thrombin light chain
Thrombin heavy chain
Coagulation factor II
P00734
THRB_HUMAN
PROTHROMBIN PRECURSOR (EC 3.4.21.5) (COAGULATION FACTOR II). [SOURCE:UNIPROT/SWISSPROT;ACC:P00734]
PA157
Coagulation factor IIa
T94033

Gene Info:

Interpro Acc	IPR001254
Human Readable Name	DRUGGABLE GENOME
Uniprot Evidence	1: Evidence at protein level
Interpro Short Name	Peptidase_S1_S6
Interpro Name	Peptidase S1/S6, chymotrypsin/Hap
Interpro Type	Domain
Uniprot Status	Swiss-Prot
Human Readable Name	PROTEASE
Target Class	Enzymes
Target Subclass	EC:3.4.21.5
Target Subclass	3.4.21.5
Target Main Class	Enzymes
Gene Biotype	PROTEIN_CODING

(9 More Sources)

Gene Categories: Category Details

GROWTH FACTOR
PROTEASE
EXTERNAL SIDE OF PLASMA MEMBRANE
DRUGGABLE GENOME

Publications:

Eriksson, 2000, New therapeutic options in deep vein thrombosis prophylaxis., Semin. Hematol.
Turpie, 1999, Anticoagulants in acute coronary syndromes., Am. J. Cardiol.
Fabrizio, 2001, Use of ecarin clotting time (ECT) with lepirudin therapy in heparin-induced thrombocytopenia and cardiopulmonary bypass., J Extra Corpor Technol
Szaba et al., 2002, Roles for thrombin and fibrin(ogen) in cytokine/chemokine production and macrophage adhesion in vivo., Blood
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Warkentin, 2000, Venous thromboembolism in heparin-induced thrombocytopenia., Curr Opin Pulm Med
Serebruany et al., 1998, A Randomized, Blinded Study of Two Doses of Novastan(R) (Brand of Argatroban) Versus Heparin as Adjunctive Therapy to Recombinant Tissue Plasminogen Activator (Accelerated Administration) in Acute Myocardial Infarction: Rationale and Design of the Myocardial Infarction using Novastan(R) and T-PA (MINT) Study., J. Thromb. Thrombolysis
Sakai et al., 1999, Argatroban as a potential anticoagulant in cardiopulmonary bypass-studies in a dog model., Cardiovasc Surg
Jang et al., 1999, A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study., J. Am. Coll. Cardiol.
Matsuo et al., 1995, Effect of Thrombin Inhibition on Patients with Peripheral Arterial Obstructive Disease: A Multicenter Clinical Trial of Argatroban., J. Thromb. Thrombolysis
Kawada et al., 1999, Argatroban, an attractive anticoagulant, for left heart bypass with centrifugal pump for repair of traumatic aortic rupture., Jpn. J. Thorac. Cardiovasc. Surg.
Gladwell, 2002, Bivalirudin: a direct thrombin inhibitor., Clin Ther
Carswell et al., 2002, Bivalirudin: a review of its potential place in the management of acute coronary syndromes., Drugs
Kleiman et al., 2002, Pharmacodynamic profile of the direct thrombin antagonist bivalirudin given in combination with the glycoprotein IIb/IIIa antagonist eptifibatide., Am. Heart J.
Bates, 2001, Bivalirudin for percutaneous coronary intervention and in acute coronary syndromes., Curr Cardiol Rep
Scatena, 2000, Bivalirudin: a new generation antithrombotic drug., Expert Opin Investig Drugs
Testa et al., 2007, The direct thrombin inhibitor ximelagatran/melagatran: a systematic review on clinical applications and an evidence based assessment of risk benefit profile., Expert Opin Drug Saf
Ersdal et al., 2005, No influence of food on the pharmacokinetics, pharmacodynamics or tolerability of the 24mg and 36mg oral tablet formulations of ximelagatran., Clin Drug Investig
Bergqvist et al., 2004, Pharmacokinetics, preliminary efficacy and safety of subcutaneous melagatran and oral ximelagatran : a multicentre study of thromboprophylaxis in elective abdominal surgery., Clin Drug Investig
Ho et al., 2006, Ximelagatran: direct thrombin inhibitor., Vasc Health Risk Manag
McCarthy et al., 1989, Retinoid-induced hemorrhaging and bone toxicity in rats fed diets deficient in vitamin K., Toxicol. Appl. Pharmacol.
Casper et al., 1989, Evaluation of vitamin K3 feed additive for prevention of sweet clover disease., J. Vet. Diagn. Invest.
Lee et al., 1999, Advantages of calcium green-1 over other fluorescent dyes in measuring cytosolic calcium in platelets., Anal. Biochem.
Wang et al., 1995, The growth inhibitory effects of vitamins K and their actions on gene expression., Hepatology
Szejtli et al., 1983, Preparation, properties and biological activity of beta-cyclodextrin inclusion complex of menadione., Pharmazie
Blackburn C et al., 2010, Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome., Bioorg Med Chem Lett
Luesch H et al., 2000, Apramides A-G, novel lipopeptides from the marine cyanobacterium Lyngbya majuscula., J Nat Prod

BIVALIRUDIN F2

Interaction Score: 21.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name bivalirudin,Angiomax, Angiox

Novel drug target Established target

Mechanism of Interaction Thrombin inhibitor

PMIDs:
11833835 11929334 11752352 11923794 11504570 11060732

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
XIMELAGATRAN F2

Interaction Score: 14.92

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17688383 17532684 17516699 11752352 17319469

Sources:
TdgClinicalTrial TEND
ARGATROBAN F2

Interaction Score: 9.59

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Argatroban

Mechanism of Interaction Thrombin inhibitor

PMIDs:
10608050 10353669 10362188 11752352 10608016 10226408

Sources:
TdgClinicalTrial ChemblInteractions TTD
LEPIRUDIN F2

Interaction Score: 7.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name lepirudin (rDNA) for injection,Refludan

Novel drug target Established target

Direct Interaction yes

PMIDs:
11055889 10505536 11467439 11807012 11752352 10912644

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
APRAMIDE A F2

Interaction Score: 4.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10978206

Sources:
DTC
ODIPARCIL F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL1083499 F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CYANIN F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DABIGATRAN ETEXILATE MESYLATE F2

Interaction Score: 2.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Thrombin inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PEGMUSIRUDIN F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL586628 F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DESIRUDIN F2

Interaction Score: 2.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Thrombin inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
CYANIDIN F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ATECEGATRAN METOXIL F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name AZD-0837

PMIDs:
None found

Sources:
TdgClinicalTrial
AZD-8165 F2

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DABIGATRAN F2

Interaction Score: 0.95

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Dabigatran

Novel drug target Established target

Mechanism of Interaction Thrombin inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
LUSUTROMBOPAG F2

Interaction Score: 0.71

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
ENOXAPARIN F2

Interaction Score: 0.71

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Lovenox

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
AVATROMBOPAG F2

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
MENADIONE F2

Interaction Score: 0.46

Interaction Types & Directionality:

activator (activating)

Interaction Info:

PMIDs:
2922761 2484931 10469489 7657295 6867080

Sources:
TEND
MELAGATRAN F2

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
ANISINDIONE F2

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CIANIDANOL F2

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
(-)-EPICATECHIN F2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SILIBININ F2

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
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
TAMOXIFEN F2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
BORTEZOMIB F2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
QUERCETIN F2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

Ensembl: ENSG00000180210
- Version: 101_38
Alternate Names:

F2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P00734
- Version: 11-September-2012
Alternate Names:

THRB_HUMAN Uniprot Id

PROTHROMBIN Uniprot Protein Name

P00734 Uniprot Accession

Gene Info:

Interpro Acc IPR001254

Human Readable Name DRUGGABLE GENOME

Uniprot Evidence 1: Evidence at protein level

Gene Categories:

PROTEASE, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000180210
- Version: 26-July-2011
Alternate Names:

PROTHROMBIN PRECURSOR (EC 3.4.21.5) (COAGULATION FACTOR II). [SOURCE:UNIPROT/SWISSPROT;ACC:P00734] Description

F2 Display Id

ENSG00000180210 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P00734
- Version: January-2014
Alternate Names:

F2 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:3.4.21.5

Publications:
TEND: P00734
- Version: 01-August-2011
Alternate Names:

2147 Entrez Gene Id

F2 Gene Symbol

ENSG00000180210 Ensembl Gene Id

Gene Info:

Target Subclass 3.4.21.5

Target Main Class Enzymes

Publications:

PharmGKB: F2

Version: 18-August-2020

Alternate Names:

PA157 PharmGKB ID

Gene Info:

Publications:

Sidney S et al., 2004, Venous thromboembolic disease in users of low-estrogen combined estrogen-progestin oral contraceptives., Contraception

McDaid A et al., 2017, Risk prediction of developing venous thrombosis in combined oral contraceptive users., PLoS One

Legnani C et al., 2002, Venous thromboembolism in young women; role of thrombophilic mutations and oral contraceptive use., Eur Heart J

TTD: Coagulation factor IIa

Version: 2020.06.01

Alternate Names:

F2 TTD Gene Abbreviation

T94033 TTD Target ID

Gene Info:

Publications:

Salas CM et al., 2013, Antithrombin III Utilization in a Large Teaching Hospital., P T

Ni X et al., 2011, Nucleic acid aptamers: clinical applications and promising new horizons., Curr Med Chem

DTC: F2

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Luesch H et al., 2000, Apramides A-G, novel lipopeptides from the marine cyanobacterium Lyngbya majuscula., J Nat Prod

Blackburn C et al., 2010, Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome., Bioorg Med Chem Lett

ChemblInteractions: F2
- Version: chembl_23
Alternate Names:

F2 GENE_SYMBOL

Prothrombin UNIPROT

Activation peptide fragment 1 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000180210
- Version: 31-May-2017
Alternate Names:

ENSG00000180210 Gene Symbol

F2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: F2
- Version: 27-Jun-2013
Alternate Names:

2147 Gene ID

PT dGene Synonym

RPRGL2 dGene Synonym

Gene Info:

Gene Categories:

PROTEASE

Publications:
GO: F2
- Version: 01-February-2022
Alternate Names:

Gene Info:

Gene Categories:

GROWTH FACTOR, EXTERNAL SIDE OF PLASMA MEMBRANE

Publications:
FDA: F2
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:

Trial Name	bivalirudin,Angiomax, Angiox
Novel drug target	Established target
Mechanism of Interaction	Thrombin inhibitor

Trial Name	lepirudin (rDNA) for injection,Refludan
Novel drug target	Established target
Direct Interaction	yes

Trial Name	Dabigatran
Novel drug target	Established target
Mechanism of Interaction	Thrombin inhibitor

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

THRB_HUMAN	Uniprot Id
PROTHROMBIN	Uniprot Protein Name
P00734	Uniprot Accession

PROTHROMBIN PRECURSOR (EC 3.4.21.5) (COAGULATION FACTOR II). [SOURCE:UNIPROT/SWISSPROT;ACC:P00734]	Description
F2	Display Id
ENSG00000180210	Ensembl Gene Id

2147	Entrez Gene Id
F2	Gene Symbol
ENSG00000180210	Ensembl Gene Id

F2	GENE_SYMBOL
Prothrombin	UNIPROT
Activation peptide fragment 1	UNIPROT

F2 Gene Record

F2 2147 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name bivalirudin,Angiomax, Angiox Novel drug target Established target Mechanism of Interaction Thrombin inhibitor

PMIDs: 11833835 11929334 11752352 11923794 11504570 11060732

Sources: TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17688383 17532684 17516699 11752352 17319469

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name Argatroban Mechanism of Interaction Thrombin inhibitor

PMIDs: 10608050 10353669 10362188 11752352 10608016 10226408

Sources: TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name lepirudin (rDNA) for injection,Refludan Novel drug target Established target Direct Interaction yes

PMIDs: 11055889 10505536 11467439 11807012 11752352 10912644

Sources: TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10978206

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Thrombin inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Thrombin inhibitor

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name AZD-0837

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Dabigatran Novel drug target Established target Mechanism of Interaction Thrombin inhibitor

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info: Trial Name Lovenox Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name bivalirudin,Angiomax, Angiox

Novel drug target Established target

Mechanism of Interaction Thrombin inhibitor

PMIDs:
11833835 11929334 11752352 11923794 11504570 11060732

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17688383 17532684 17516699 11752352 17319469

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Argatroban

Mechanism of Interaction Thrombin inhibitor

PMIDs:
10608050 10353669 10362188 11752352 10608016 10226408

Sources:
TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name lepirudin (rDNA) for injection,Refludan

Novel drug target Established target

Direct Interaction yes

PMIDs:
11055889 10505536 11467439 11807012 11752352 10912644

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
10978206

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Thrombin inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Thrombin inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name AZD-0837

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Dabigatran

Novel drug target Established target

Mechanism of Interaction Thrombin inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Lovenox

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB FDA

Interaction Types & Directionality:

activator (activating)

PMIDs:
2922761 2484931 10469489 7657295 6867080

Sources:
TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found