Target Information
Target General Infomation | |||||
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Target ID |
T83369
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Former ID |
TTDC00078
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Target Name |
Coagulation factor IX
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Gene Name |
F9
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Synonyms |
Christmas factor; Factor IX; PTC; Plasma thromboplastin component; F9
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Target Type |
Successful
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Disease | Blood forming organ disorders [ICD10: D75.9] | ||||
Factor IX deficiency [ICD10: D67] | |||||
Factor IX deficiency; Haemophilia B [ICD9:286.1; ICD10: D67] | |||||
Hemophilia A [ICD9: 286; ICD10: D66] | |||||
Hemophilia [ICD9: 286; ICD10: D66-D68] | |||||
Sepsis [ICD9: 995.91; ICD10: A40, A41] | |||||
Thrombosis; Coronary artery disease; Vascular diseases [ICD9: 325, 410-414, 429.2, 430-459, 437.6, 453, 671.5, 671.9; ICD10: G45-G46, I20-I25, I60-I95, I80-I82] | |||||
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
Unspecified [ICD code not available] | |||||
Function |
Factor IX is a vitamin K-dependent plasma protein that participates in the intrinsic pathway of blood coagulation by converting factor X to its active form in the presence of Ca(2+) ions, phospholipids, and factor VIIIa.
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BioChemical Class |
Peptidase
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Target Validation |
T83369
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UniProt ID | |||||
EC Number |
EC 3.4.21.22
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Sequence |
MQRVNMIMAESPGLITICLLGYLLSAECTVFLDHENANKILNRPKRYNSGKLEEFVQGNL
ERECMEEKCSFEEAREVFENTERTTEFWKQYVDGDQCESNPCLNGGSCKDDINSYECWCP FGFEGKNCELDVTCNIKNGRCEQFCKNSADNKVVCSCTEGYRLAENQKSCEPAVPFPCGR VSVSQTSKLTRAETVFPDVDYVNSTEAETILDNITQSTQSFNDFTRVVGGEDAKPGQFPW QVVLNGKVDAFCGGSIVNEKWIVTAAHCVETGVKITVVAGEHNIEETEHTEQKRNVIRII PHHNYNAAINKYNHDIALLELDEPLVLNSYVTPICIADKEYTNIFLKFGSGYVSGWGRVF HKGRSALVLQYLRVPLVDRATCLRSTKFTIYNNMFCAGFHEGGRDSCQGDSGGPHVTEVE GTSFLTGIISWGEECAMKGKYGIYTKVSRYVNWIKEKTKLT |
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Drugs and Mode of Action | |||||
Drug(s) | CSL-654 | Drug Info | Phase 3 | Factor IX deficiency | [524630] |
TTP889 | Drug Info | Phase 2 | Blood forming organ disorders | [536572] | |
AMT-060 | Drug Info | Phase 1/2 | Factor IX deficiency | [548603] | |
RG6013 | Drug Info | Phase 1/2 | Hemophilia A | [549416] | |
AAV2-hFIX16 | Drug Info | Phase 1 | Factor IX deficiency | [522086] | |
N9-GP | Drug Info | Phase 1 | Factor IX deficiency; Haemophilia B | [523545] | |
RB-006 | Drug Info | Discontinued in Phase 3 | Thrombosis; Coronary artery disease; Vascular diseases | [547853] | |
Trenonacog alfa | Drug Info | Discontinued in Phase 3 | Unspecified | [1559854] | |
SB 249417 | Drug Info | Discontinued in Phase 1 | Sepsis | [546894] | |
Draculin | Drug Info | Terminated | Thrombosis | [545778] | |
Recombinant Factor IX | Drug Info | Terminated | Factor IX deficiency | [549852] | |
Inhibitor | 2-amidino-4-iodobenzothiophene | Drug Info | [530682] | ||
4-Benzyloxybenzo[b]thiophene-2-carboxamidine | Drug Info | [530682] | |||
4-Phenyl-benzo[b]thiophene-2-carboxamidine | Drug Info | [530682] | |||
5-Benzyloxy-benzo[b]thiophene-2-carboxamidine | Drug Info | [530682] | |||
6-Benzyloxybenzo[b]thiophene-2-carboxamidine | Drug Info | [530682] | |||
compound 57 | Drug Info | [530681] | |||
Gamma-Carboxy-Glutamic Acid | Drug Info | [551393] | |||
RAZAXABAN | Drug Info | [527987] | |||
RB-006 | Drug Info | [537273] | |||
TTP889 | Drug Info | [536262], [536572] | |||
Modulator | AAV2-hFIX16 | Drug Info | [544166] | ||
AMT-060 | Drug Info | [550344] | |||
BNP-FIX | Drug Info | [543608] | |||
CSL-654 | Drug Info | [544258] | |||
Draculin | Drug Info | [534730] | |||
F-9TG | Drug Info | [543608] | |||
Factor IX-XTEN | Drug Info | [543608] | |||
MG-1104 | Drug Info | [543608] | |||
MOD-3012 | Drug Info | [543608] | |||
N9-GP | Drug Info | [531467] | |||
Recombinant Factor IX | Drug Info | [532997] | |||
Trenonacog alfa | Drug Info | ||||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Complement and coagulation cascades | ||||
PANTHER Pathway | Blood coagulation | ||||
PathWhiz Pathway | Coagulation | ||||
Reactome | Extrinsic Pathway of Fibrin Clot Formation | ||||
Intrinsic Pathway of Fibrin Clot Formation | |||||
Gamma-carboxylation of protein precursors | |||||
Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus | |||||
Removal of aminoterminal propeptides from gamma-carboxylated proteins | |||||
WikiPathways | Complement and Coagulation Cascades | ||||
gamma carboxylation, hypusine formation and arylsulfatase activation | |||||
Blood Clotting Cascade | |||||
Formation of Fibrin Clot (Clotting Cascade) | |||||
References | |||||
Ref 522086 | ClinicalTrials.gov (NCT00515710) LTFU for Gene Transfer Subjects With Hemophilia B. U.S. National Institutes of Health. | ||||
Ref 523545 | ClinicalTrials.gov (NCT01395810) Safety and Efficacy of NNC-0156-0000-0009 After Long-Term Exposure in Patients With Haemophilia B: An Extension to Trials NN7999-3747 and NN7999-3773. U.S. National Institutes of Health. | ||||
Ref 524630 | ClinicalTrials.gov (NCT02053792) A Safety and Efficacy Extension Study of a Recombinant Fusion Protein Linking Coagulation Factor IX With Albumin (rIX-FP) in Patients With Hemophilia B. U.S. NationalInstitutes of Health. | ||||
Ref 536572 | Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study. J Thromb Haemost. 2008 Mar;6(3):457-63. Epub 2007 Dec 12. | ||||
Ref 545778 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004668) | ||||
Ref 546894 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010912) | ||||
Ref 547853 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019932) | ||||
Ref 548603 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026919) | ||||
Ref 526314 | Pharmacokinetic and pharmacodynamic modeling of humanized anti-factor IX antibody (SB 249417) in humans. Clin Pharmacol Ther. 2002 Apr;71(4):235-45. | ||||
Ref 527987 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):1795-8. Epub 2006 Jan 24.Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors. | ||||
Ref 530681 | Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors. J Med Chem. 2010 Feb 25;53(4):1473-82. | ||||
Ref 530682 | J Med Chem. 2010 Feb 25;53(4):1465-72.Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis. | ||||
Ref 531467 | Enhanced pharmacokinetic properties of a glycoPEGylated recombinant factor IX: a first human dose trial in patients with hemophilia B. Blood. 2011 Sep 8;118(10):2695-701. | ||||
Ref 532739 | Anti-factor IXa/X bispecific antibody (ACE910): hemostatic potency against ongoing bleeds in a hemophilia A model and the possibility of routine supplementation. J Thromb Haemost. 2014 Feb;12(2):206-13. | ||||
Ref 532997 | BAX326 (RIXUBIS): a novel recombinant factor IX for the control and prevention of bleeding episodes in adults and children with hemophilia B. Ther Adv Hematol. 2014 Oct;5(5):168-80. | ||||
Ref 534730 | Expression of biological activity of draculin, the anticoagulant factor from vampire bat saliva, is strictly dependent on the appropriate glycosylation of the native molecule. Biochim Biophys Acta. 1998 Oct 23;1425(2):291-9. | ||||
Ref 536262 | Oral anticoagulants in development: focus on thromboprophylaxis in patients undergoing orthopaedic surgery. Drugs. 2006;66(11):1411-29. | ||||
Ref 536572 | Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study. J Thromb Haemost. 2008 Mar;6(3):457-63. Epub 2007 Dec 12. | ||||
Ref 537273 | In-vitro evaluation of anti-factor IXa aptamer on thrombin generation, clotting time, and viscoelastometry. Thromb Haemost. 2009 May;101(5):827-33. | ||||
Ref 543608 | (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: 2364). | ||||
Ref 544166 | Assessing the potential for AAV vector genotoxicity in a murine model. Correction in: Blood. 2011 June 16; 117(24): 6739. |
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