RCSB PDB - 3LC5: Selective Benzothiophine Inhibitors of Factor IXa
Structure Based Drug Design: Development of Potent and Selective Factor IXa (FIXa) Inhibitors.. Wang, S., Beck, R., Burd, A., ... A number of highly selective and potent factor Xa (FXa) and FIXa inhibitors were identified by simple switch of functional ... Selective Benzothiophine Inhibitors of Factor IXa. *PDB DOI: https://doi.org/10.2210/pdb3LC5/pdb ...
JCI - Active site-blocked factor IXa prevents intravascular thrombus formation in the coronary vasculature without inhibiting...
... bovine glutamyl-glycyl-arginyl-Factor IXa (IXai), a competitive inhibitor of Factor IXa assembly into the intrinsic Factor X ... This suggests that Factor IX/IXa can contribute to thrombus formation, and that inhibition of IXa participation in the clotting ... Active site-blocked factor IXa prevents intravascular thrombus formation in the coronary vasculature without inhibiting ... To assess the contribution of Factor IX/IXa, to intravascular thrombosis, a canine coronary thrombosis model was studied. ...
Human Factor IXa, biotinylated EGR - CellSystems®
Factor IXa is not inhibited by DFP. Factor IXa is prepared from highly purified factor IX by activation with factor XIa, as ... Factor IXa is produced from its inactive precursor, factor IX, via proteolytic cleavage by factor XIa or the tissue factor/ ... Factor IXa functions as a serine protease involved in the activation of the zymogen, factor X, to form the enzyme, factor Xa. ... 5). The factor IXa is further purified by gel filtration, followed by immunoaffinity purification. Factor IXa is also available ...
Bovine Factor IXa - blocked active site (EGRck)
Human Factor IXa Human Factor IXa - blocked active site (DEGRck) Human Factor IXa - blocked active site (EGRck) Rat Factor IXa ... Bovine Factor IXa Bovine Factor IXa - blocked active site (DEGRck) ... 1 % activity IXa - Active-site blocked MW(Da) : 45 000 Extinction coef. : 14 Structure: 2 subunits (MW(Da) : 28 000 & 17 000 ...
Factor ixa; Factor IX, Activated; Coagulation Factor IXa
Factor IX, Activated; Coagulation Factor IXa. On-line free medical diagnosis assistant. Ranked list of possible diseases from ... Factor ixa (Factor IX, Activated; Coagulation Factor IXa). Activated form of factor IX. This activation can take place via the ... factor ixa serves to activate factor X to Xa by cleaving the arginyl-leucine peptide bond in factor X. ... intrinsic pathway by the action of factor xia and calcium, or via the extrinsic pathway by the action of factor viia, ...
Antidote-controlled antithrombotic therapy targeting factor IXa and von Willebrand factor.
"Antidote-controlled antithrombotic therapy targeting factor IXa and von Willebrand factor." Ann N Y Acad Sci, vol. 1175, Sept. ... "Antidote-controlled antithrombotic therapy targeting factor IXa and von Willebrand factor." Ann N Y Acad Sci 1175 (September ... Antidote-controlled antithrombotic therapy targeting factor IXa and von Willebrand factor.. Publication , Journal Article ... Antidote-controlled antithrombotic therapy targeting factor IXa and von Willebrand factor. Ann N Y Acad Sci, 1175, 61-70. https ...
REG1 - Wikipedia
REG1 mechanism of action It involves inhibition of Factor IXa. REG1 is being developed for use in patients undergoing ... Becker RC, Chan MY (December 2009). "REG-1, a regimen comprising RB-006, a Factor IXa antagonist, and its oligonucleotide ... a single-stranded 31-nucleotide aptamer that binds and inhibits Factor IXa, and anivamersen, a complementary sequence reversal ... Vavalle, John Paul; Cohen, Mauricio G (2012). "The REG1 anticoagulation system: a novel actively controlled factor IX inhibitor ...
Factor VII Deficiency: Practice Essentials, Background, Pathophysiology
Factor VII/tissue factor complex activates factor IX and factor X. Factor IXa along with factor VIIIa results in formation of ... Factor VII/tissue factor complex activates factor IX and factor X. Factor IXa along with factor VIIIa results in formation of ... factor IXa, factor Xa, factor XIa, and factor XIIa. Comparison of these proteins has shown that factor Xa, in association with ... Activation of factor X by the factor VIIa-tissue factor complex results in the interaction of factor Xa with factor Va to form ...
SCOPe 2.08: Domain d1edmb : 1edm B
FS Robert Theobald, Jr.
SMART: EGF CA domain annotation
Porcine Factor IXa Complexed to 1-{3-[amino(imino)methyl]phenyl}-N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-3-(trifluoromethyl ... Human factor viia-tissue factor complexed with highly selective peptide inhibitor. 2zzu. Human Factor VIIA-Tissue Factor ... COAGULATION FACTOR, NMR, 15 STRUCTURES. 1wqv. Human Factor Viia-Tissue Factor Complexed with propylsulfonamide-D-Thr-Met-p- ... Crystal Structure of Benzamidine-Factor VIIa/Soluble Tissue Factor complex.. 2b7d. Factor VIIa Inhibitors: Chemical ...
SMART: EGF CA domain annotation
Porcine Factor IXa Complexed to 1-{3-[amino(imino)methyl]phenyl}-N-[4-(1H-benzimidazol-1-yl)-2-fluorophenyl]-3-(trifluoromethyl ... Human factor viia-tissue factor complexed with highly selective peptide inhibitor. 2zzu. Human Factor VIIA-Tissue Factor ... COAGULATION FACTOR, NMR, 15 STRUCTURES. 1wqv. Human Factor Viia-Tissue Factor Complexed with propylsulfonamide-D-Thr-Met-p- ... Crystal Structure of Benzamidine-Factor VIIa/Soluble Tissue Factor complex.. 2b7d. Factor VIIa Inhibitors: Chemical ...
Bengt Eriksson | University of Gothenburg
Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study ... Oral, direct Factor Xa inhibition with BAY 59-7939 for the prevention of venous thromboembolism after total hip replacement ... A dose-finding study with TAK-442, an oral factor Xa inhibitor, in patients undergoing elective total knee replacement surgery ... Novel oral factor Xa and thrombin inhibitors in the management of thromboembolism. ...
Hemophilia A (Factor VIII Deficiency): Practice Essentials, Background, Pathophysiology
... recessive disorder caused by deficiency of functional plasma clotting factor VIII (FVIII). In a significant number of cases, ... TF also adsorbs factor X to enhance the reaction between factor VIIa, factor X, and calcium ions. Factor IXa and factor XII ... Factor IXa can bind phospholipids. Then, factor X is activated on the phospholipid surface; activation of factor X involves a ... In the extrinsic system, the conversion of factor X to factor Xa involves tissue factor (TF), or thromboplastin; factor VII; ...
Isleen Sheares's Presentations on SlideServe
Deep Venous Thrombosis Prophylaxis in Orthopedic Surgery: Background, Mechanical Methods, Pharmacologic Methods
... catalyzes the inactivation of factors IIa, Xa, IXa, and XIIa. ... Table 2. Deep Venous Thrombosis Risk Factor Scores Risk Factor ... Risk factors are grouped according to severity and are added to produce an overall risk factor score, which corresponds to a ... Additional risk factors may include a history of VTE, malignancy, or hypercoagulable state. These factors carry an estimated ... heparin not only prevents fibrin formation but also inhibits thrombin-induced activation of factor V and factor VIII. Of these ...
RX List database - use generic or medication brand name - GlobalRPH
Factor IX preactivation, the percent of Factor IXa/Factor IX as measured by activity assays, is ≤ 0.03%. The potency in ... Monitor factor IX activity plasma levels by the one-stage clotting assay to confirm that adequate factor IX levels have been ... b Calculated as (Cmax - baseline factor IX) divided by the dose in IU/kg, where Cmax is the maximum post-infusion factor IX ... a Calculated as (C30min-baseline factor IX) divided by the dose in IU/kg, where C30min is the factor IX measurement 30 minutes ...
KAKEN - Researchers | Takeyama Masahiro (30572010)
Presentation] Contribution of Factor VIII A3 Domain Residues 1793-1795 to a Factor IXa-Interactive Site2018. *. Author(s). ... Journal Article] An anti-factor IXa/factor X bispecific antibody, emicizumab, improves ex vivo coagulant potentials in plasma ... Presentation] Anti-Factor IXa/FX antibody (ACE910) improves the coagulation function in acquired hemophilia A ex vivo.2015. *. ... Presentation] Factor VIII A2 domain contains a binding site for factor X. *. Author(s). Masahiro Takeyama, Keiji Nogami, Tomoko ...
Federal Circuit Evaluates Enablement for Antibody Claims for the First Time Since Amgen v. Sanofi in Baxalta Inc. et al. v....
... antibody or antibody fragment thereof that binds Factor IX or Factor IXa and increases the procoagulant activity of Factor IXa. ... Factors IX and IXa) to yield a functional result (an increase of pro-coagulant activity of Factor IXa): ... claims describe all antibodies that bind to Factor IX/IXa and functionally increase the pro-coagulant activity of Factor IXa. ... goes on to explain how the inventors screened the antibodies they generated to identify those that bind to Factors IX/IXa and ...
Hypercoagulable Disorders
... the activity of activated clotting factors Xa, IXa, XIa, and thrombin. Deficiency can lead to a clot formation. ... Factor V Leiden is a condition caused by mutation in Factor V(F5) gene at position 1691, increasing the risk of Deep Vein ... This increases the circulating level of Factor II (thrombin) which is a major factor in the clotting cascade at promoting ... the activity of factor VIIIa and factor Va. Deficiency can lead to increased clot formation and more serious complications as ...
Frontiers | Platelet Membrane Receptor Proteolysis: Implications for Platelet Function
... factor XIa cleaves factor IX, but so far, no proteolytic events of factor IXa or XIa on platelet membrane proteins have been ... with as protease factor IXa and as cofactor VIIIa, catalyzes the conversion of factor X into factor Xa. Subsequently, the ... the protease factor Xa is produced from its zymogen factor X by factor VII/VIIa (1, 9). Cleavage into factor Xa is greatly ... Tissue factor- and factor X- dependent activation of protease-activated receptor 2 by factor VIIa. Proc Natl Acad Sci USA. ( ...
SMART: FA58C domain annotation
The effective activation of factor X by factor IXa requires the co-factor activity of activated factor VIII (FVIII). Factor Xa ... Synthetic factor VIII peptides with amino acid sequences contained within the C2 domain of factor VIII inhibit factor VIII ... Cloning of a cDNA coding for human factor V, a blood coagulation factor homologous to factor VIII and ceruloplasmin. ... identity with the corresponding domains in factor VIII. As in factor VIII, the A domains of factor V share approximately 40% ...
Hemlibra (Emicizumab-Kxwh Injection, for Subcutaneous Use): Uses, Dosage, Side Effects, Interactions, Warning
Emicizumab-kxwh is a humanized monoclonal modified immunoglobulin G4 (IgG4) bispecific antibody binding factor IXa and factor X ... Hemlibra (emicizumab-kxwh) injection is a bispecific factor IXa- and factor X-directed antibody indicated for routine ... HEMLIBRA bridges activated factor IX and factor X to restore the function of missing activated factor VIII that is needed for ... Hemophilia A is a bleeding condition people can be born with where a missing or faulty blood clotting factor (factor VIII) ...
A Phase 2, Randomized, Partially Blinded, Active-Controlled Study Assessing the Efficacy and Safety of Variable Anticoagulation...
Keywords: Odds Ratio, Aptamers, Nucleotide, Acute Coronary Syndrome, Myocardial Infarction, Factor IXa, Cardiac Catheterization ... Adequately powered randomized clinical trials are indicated to determine the safety and efficacy of factor IXa inhibition with ... This study suggests that near complete inhibition of factor IXa with pegnivacogin, followed by anivamersen-mediated reversal, ...
Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents and Patent Applications (Class 548/241) - Justia...
FACTOR IXA INHIBITORS Publication number: 20140219989 Abstract: The present invention provides a compound of Formula (I) as ... The benzo[d]oxazole derivative, which is a nuclear factor E2-related factor 2 (Nrf2) inhibitor, is capable of inhibiting ... Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced ...
Roche 2018: Personalized healthcare focus - PharmaLive
The bispecific factor IXa- and factor X-directed antibody is available in the United States for patients with hemophilia A with ... Hemlibra is designed to bring together factor IXa and factor X, proteins necessary to activate the natural coagulation cascade ... for routine prophylaxis of bleeding episodes in people with hemophilia A with factor VIII inhibitors and can be used in all age ... the development of factor VIII inhibitors, and the need for frequent venous access. ...
Jonathan M. Chen, MD | Children's Hospital of Philadelphia
Selective anticoagulation with active site blocked factor IXa (IXai) implicates distinct roles for intrinsic and extrinsic ... Age less than two years is not a risk factor for mortality after mitral valve replacement in children. Ann Thorac Surg 2011; ... Russo MJ, Iribarne A, Hong KN, Ramlawi B, Chen JM, Takayama H, Mancini DM, Naka Y. Factors associated with primary graft ... Multiple risk factors before pediatric cardiac transplantation are associated with increased graft loss. Pediatric Cardiol 2011 ...
BIOPHEN™ FIXa (ACT. FIX) | Quadratech Diagnostics
Paper | Ixa taldea
Sir James Black Drug Discovery of the Year | British Pharmacological Society