Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T43332
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| Former ID |
TTDR00947
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| Target Name |
Coagulation factor VII
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| Gene Name |
F7
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| Synonyms |
Eptacog alfa; Factor VII; Proconvertin; SPCA; Serum prothrombin conversion accelerator; F7
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| Target Type |
Successful
|
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| Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
| Bleeding [ICD9: 444, 453; ICD10: I74, I80-I82] | |||||
| Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
| Factor IX deficiency [ICD10: D67] | |||||
| Factor VII deficiency [ICD10: D68] | |||||
| Hemophilia [ICD9: 286; ICD10: D66-D68] | |||||
| Function |
Initiates the extrinsic pathway of bloodcoagulation. Serine protease that circulates in the blood in a zymogen form. Factor VII is converted to factor VIIa by factor Xa, factor XIIa, factor IXa, or thrombin by minor proteolysis. In the presence of tissue factor and calcium ions, factor VIIa then converts factor X to factor Xa by limited proteolysis. Factor VIIa will also convert factor IX to factor IXa in the presence of tissue factor and calcium.
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| BioChemical Class |
Peptidase
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| Target Validation |
T43332
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| UniProt ID | |||||
| EC Number |
EC 3.4.21.21
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| Sequence |
MVSQALRLLCLLLGLQGCLAAGGVAKASGGETRDMPWKPGPHRVFVTQEEAHGVLHRRRR
ANAFLEELRPGSLERECKEEQCSFEEAREIFKDAERTKLFWISYSDGDQCASSPCQNGGS CKDQLQSYICFCLPAFEGRNCETHKDDQLICVNENGGCEQYCSDHTGTKRSCRCHEGYSL LADGVSCTPTVEYPCGKIPILEKRNASKPQGRIVGGKVCPKGECPWQVLLLVNGAQLCGG TLINTIWVVSAAHCFDKIKNWRNLIAVLGEHDLSEHDGDEQSRRVAQVIIPSTYVPGTTN HDIALLRLHQPVVLTDHVVPLCLPERTFSERTLAFVRFSLVSGWGQLLDRGATALELMVL NVPRLMTQDCLQQSRKVGDSPNITEYMFCAGYSDGSKDSCKGDSGGPHATHYRGTWYLTG IVSWGQGCATVGHFGVYTRVSQYIEWLQKLMRSEPRPGVLLRAPFP |
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| Drugs and Mode of Action | |||||
| Drug(s) | Factor viia | Drug Info | Approved | Hemophilia | [1] |
| BAX-817 | Drug Info | Phase 3 | Hemophilia | [2] | |
| Vatreptacog alfa (activated) | Drug Info | Phase 3 | Bleeding | [3] | |
| Activated recombinant FVII-albumin fusion protein | Drug Info | Phase 2/3 | Hemophilia | [4] | |
| Recombinant factor VIIa PEGylated liposomal | Drug Info | Phase 1/2 | Factor VII deficiency | [5] | |
| CB-813 | Drug Info | Phase 1 | Hemophilia | [6] | |
| Eptacog alfa intravenous | Drug Info | Phase 1 | Hemophilia | [7] | |
| F-7TG | Drug Info | Phase 1 | Hemophilia | [8] | |
| compound 1 | Drug Info | Clinical trial | Alzheimer disease | [9], [10] | |
| BAY 86-6150 | Drug Info | Discontinued in Phase 2/3 | Hemophilia | [11] | |
| RNAPc2 | Drug Info | Discontinued in Phase 2 | Colorectal cancer | [12] | |
| Inhibitor | 4-(3,4-Diethoxy-benzylamino)-benzamidine | Drug Info | [13] | ||
| 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine | Drug Info | [13] | |||
| BAX-817 | Drug Info | [14] | |||
| compound 1 | Drug Info | [9] | |||
| compound 11 | Drug Info | [15] | |||
| Fucose | Drug Info | [16] | |||
| Modulator | Activated recombinant FVII-albumin fusion protein | Drug Info | [17] | ||
| BAY 86-6150 | Drug Info | [18] | |||
| CB-813 | Drug Info | [19] | |||
| Eptacog alfa intravenous | Drug Info | [20] | |||
| F-7TG | Drug Info | [21] | |||
| Factor viia | Drug Info | [21] | |||
| Factor-VIIa-XTEN | Drug Info | [21] | |||
| Human recombinant factor VIIa | Drug Info | [21] | |||
| Long-acting Factor VII conjugate | Drug Info | [21] | |||
| MOD-5023 | Drug Info | [21] | |||
| Recombinant factor VIIa PEGylated liposomal | Drug Info | [21] | |||
| RNAPc2 | Drug Info | [22] | |||
| Vatreptacog alfa (activated) | Drug Info | [23] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Complement and coagulation cascades | ||||
| PANTHER Pathway | Angiogenesis | ||||
| Blood coagulation | |||||
| PathWhiz Pathway | Coagulation | ||||
| Reactome | CLOCK,NPAS2 activates circadian gene expression | ||||
| Extrinsic 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) | |||||
| Circadian Clock | |||||
| Folate Metabolism | |||||
| Vitamin B12 Metabolism | |||||
| Selenium Micronutrient Network | |||||
| References | |||||
| REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032604) | ||||
| REF 3 | ClinicalTrials.gov (NCT01392547) Efficacy and Safety of NNC 0078-0000-0007 in Patients With Congenital Haemophilia and Inhibitors. U.S. National Institutes of Health. | ||||
| REF 4 | ClinicalTrials.gov (NCT02484638) Study of Recombinant Factor VIIa Fusion Protein (rVIIa-FP, CSL689) for On-demand Treatment of Bleeding Episodes in Patients With Hemophilia A or B With Inhibitors. | ||||
| REF 5 | Safety, pharmacokinetics and efficacy of factor VIIa formulated with PEGylated liposomes in haemophilia A patients with inhibitors to factor VIII--an open label, exploratory, cross-over, phase I/II study. Haemophilia. 2010 Nov;16(6):910-8. | ||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027663) | ||||
| REF 7 | ClinicalTrials.gov (NCT02084810) Investigating the Bioequivalence of Eptacog Alfa A 6 mg and NovoSeven in Healthy Male Subjects. U.S. National Institutes of Health. | ||||
| REF 8 | GTC BIOTHERAPEUTICS REPORTS THIRD QUARTER 2010 FINANCIAL RESULTS. U.S. Securities and Exchange Commission. October 27, 2010. | ||||
| REF 9 | Efforts toward oral bioavailability in factor VIIa inhibitors. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3829-32. Epub 2006 May 2. | ||||
| REF 10 | (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: 6552). | ||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021847) | ||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006762) | ||||
| REF 13 | Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. | ||||
| REF 14 | Clinical pipeline report, company report or official report of Baxter. | ||||
| REF 15 | Small molecule inhibitors of plasma kallikrein. Bioorg Med Chem Lett. 2006 Apr 1;16(7):2034-6. Epub 2006 Jan 18. | ||||
| REF 16 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 17 | ClinicalTrials.gov (NCT01542619) A Safety and Pharmacokinetics Study of a Recombinant Fusion Protein Linking Coagulation Factor VIIa With Albumin (rVIIa-FP) in Healthy Male Volunteers. U.S. National Institutes of Health. | ||||
| REF 18 | Bayer HealthCare and Maxygen Announce Hematology Agreement. U.S. Securities and Exchange Commission. July 2, 2008. | ||||
| REF 19 | Clinical pipeline report, company report or official report of Catalyst Biosciences. | ||||
| REF 20 | Recombinant factor VIIa (eptacog alfa): a review of its use in congenital hemophilia with inhibitors, acquired hemophilia, and other congenital bleeding disorders. BioDrugs. 2008;22(2):121-36. | ||||
| REF 21 | (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: 2363). | ||||
| REF 22 | rNAPc2 inhibits colorectal cancer in mice through tissue factor. Clin Cancer Res. 2009 Jan 1;15(1):208-16. | ||||
| REF 23 | Recombinant factor VIIa analog (vatreptacog alfa [activated]) for treatment of joint bleeds in hemophilia patients with inhibitors: a randomized controlled trial. J Thromb Haemost. 2012 Jan;10(1):81-9. | ||||
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