Literature for peptidase S01.216: coagulation factor Xa

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(Topics flags: S Structure, A Assay, T Target, K Knockout, P Specificity, E Expression, V Review, M Mutation, I Inhibitor, U Therapeutic. To select only the references relevant to a single topic, click the link above. See explanation.)

2026

Banas,V., Seehra,K., Mahoney,M., Alisio,C., Kyriukha,Y., Weiland,E., Fath,M., Han,Z., Bricker,T., Tartell,M., Whelan,S., Boon,A.C.M. and Janetka,J.W. Inhibitors of membrane associated serine proteases block replication of coronavirus SARS-CoV-2 and influenza virus H1N1 Eur J Med Chem (2026) 302, 118385-118385. PubMed Europe PubMed DOI
Champagne,P.S., Seneci,L., Casewell,N.R. and Fry,B.G. Hemostatic hellfire: Rhabdophis helleri (Red-necked Keelback) snake venom pathophysiologically activates Factor VII and Factor X through novel uses of the clotting cofactors calcium, phospholipid, and Factor Va Toxicon (2026) 271, 108970-108970. PubMed Europe PubMed DOI

2025

Bozhko,A.A. and Panteleev,M.A. A mathematical model for activated platelet-dependent activation of coagulation factor X by factor IXa Comput Biol Med (2025) 192, 110263-110263. PubMed Europe PubMed DOI
Iglay,K., Aldridge,M.L., Calcinai,M., Wolford,E. and Ashrani,A.A. The global epidemiology of acquired factor X deficiency Hematology (2025) 30, 2476254-2476254. PubMed Europe PubMed DOI V
Mishima,Y., Okada,H., Butt,A.L., Stewart,K.E., Mazzeffi,M.A. and Tanaka,K.A. In vitro procoagulant effects of Gla-domainless factor Xa in factor XI-deficient and factor IX-deficient plasma Thromb Res (2025) 247, 109286-109286. PubMed Europe PubMed DOI
Ustok,F.I. and Huntington,J.A. Engineering a membrane-independent human prothrombinase through parsimonious mutation of factor Xa J Thromb Haemost (2025) PubMed Europe PubMed DOI
Ustok,F.I., Faille,A. and Huntington,J.A. A 3.3-A cryo-EM structure of an engineered high-affinity human prothrombinase complex Blood (2025) PubMed Europe PubMed DOI

2024

Al-Horani,R.A. Revisiting the effect of cholesteryl sulfate on clotting and fibrinolysis: Inhibition of human thrombin and other human blood proteases Heliyon (2024) 10, e28017-e28017. PubMed Europe PubMed DOI PMC EPMC I
Oda,A., Takeyama,M., Kitazawa,T. and Nogami,K. The emicizumab-bridged ternary complex with activated factor IX and factor X evaluated by fluorescence resonance energy transfer Thromb Res (2024) 237, 108-111. PubMed Europe PubMed DOI
Santiago,F., Kaur,A., Bride,S., Monroe,D., Leiderman,K. and Sindi,S. A new look at TFPI inhibition of factor X activation PLoS Comput Biol (2024) 20, e1012509-e1012509. PubMed Europe PubMed DOI PMC EPMC
Stojanovski,B.M., Mohammed,B.M. and Di Cera,E. The Prothrombin-Prothrombinase Interaction Subcell Biochem (2024) 104, 409-423. PubMed Europe PubMed DOI V
Zhu,B., Lane,M.D., Baller,J.A., Jagtap,P.D., Griffin,T.J. and Seelig,B. Comprehensive protease specificity profiling bioRxiv (2024) PubMed Europe PubMed DOI PMC EPMC

2023

Dong,W., Wang,J., Tian,L., Zhang,J., Settles,E.W., Qin,C., Steinken-Kollath,D.R., Itogawa,A.N., Celona,K.R., Yi,J., Bryant,M., Mead,H., Jaramillo,S.A., Lu,H., Li,A., Zumwalt,R.E., Dadwal,S., Feng,P., Yuan,W., Whelan,S.P.J., Keim,P.S., Barker,B.M., Caligiuri,M.A. and Yu,J. Factor Xa cleaves SARS-CoV-2 spike protein to block viral entry and infection Nat Commun (2023) 14, 1936-1936. PubMed Europe PubMed DOI PMC EPMC
Gackowski,M., Madriwala,B., Studzinska,R. and Koba,M. Novel Isosteviol-Based FXa Inhibitors: Molecular Modeling, In Silico Design and Docking Simulation Molecules (2023) 28 PubMed Europe PubMed DOI PMC EPMC
Lloyd,J. and Feldman,P. Preclinical development and characterization of a human plasma-derived high-purity factor X concentrate for therapeutic use Haemophilia (2023) 29, 1394-1409. PubMed Europe PubMed DOI
Novichikhina,N.P., Shestakov,A.S., Medvedeva,S.M., Lagutina,A.M., Krysin,M.Y., Podoplelova,N.A., Panteleev,M.A., Ilin,I.S., Sulimov,A.V., Tashchilova,A.S., Sulimov,V.B., Geronikaki,A. and Shikhaliev,K.S. New Hybrid Tetrahydropyrrolo[3,2,1-ij]quinolin-1-ylidene-2-thioxothiazolidin-4-ones as New Inhibitors of Factor Xa and Factor XIa: Design, Synthesis, and In Silico and Experimental Evaluation Molecules (2023) 28 PubMed Europe PubMed DOI PMC EPMC I
Wagner,N., Shayakhmetov,D.M. and Stewart,P.L. Structural Model for Factor X Inhibition of IgM and Complement-Mediated Neutralization of Adenovirus Viruses (2023) 15 PubMed Europe PubMed DOI PMC EPMC
Wang,H., Poe,A., Martinez Yus,M., Pak,L., Nandakumar,K. and Santhanam,L. Lysyl oxidase-like 2 processing by factor Xa modulates its activity and substrate preference Commun Biol (2023) 6, 375-375. PubMed Europe PubMed DOI PMC EPMC
Wu,S., Wang,T., Li,J., Zhang,Z., Li,C., Xiao,S., He,J., Wang,X., Hu,Z., Wang,X., Zheng,S., Liang,X., Chen,G., Li,Y., Li,X., Zhan,Y., Zou,Q., Jiang,H., Zheng,Q., Ban,L., Liu,H. and Fang,Y. First-in-human trial of SAR107375E, a novel small molecule anticoagulant with dual inhibition of factor Xa and factor IIa Expert Opin Investig Drugs (2023) 32, 1085-1094. PubMed Europe PubMed DOI I
Yoon,H.J., Kundu,S. and Wu,S. Molecular Dynamics Simulation Study of the Selective Inhibition of Coagulation Factor IXa over Factor Xa Molecules (2023) 28 PubMed Europe PubMed DOI PMC EPMC
Zhang,Q., Zhang,Z., Chen,W., Zheng,H., Si,D. and Zhang,W. Rivaroxaban, a direct inhibitor of coagulation factor Xa, attenuates adverse cardiac remodeling in rats by regulating the PAR-2 and TGF-beta1 signaling pathways PeerJ (2023) 11, e16097-e16097. PubMed Europe PubMed DOI PMC EPMC I

2022

Fernandez-Bachiller,M.I., Hwang,S., Schembri,M.E., Lindemann,P., Guberman,M., Herziger,S., Specker,E., Matter,H., Will,D.W., Czech,J., Wagner,M., Bauer,A., Schreuder,H., Ritter,K., Urmann,M., Wehner,V., Sun,H. and Nazare,M. Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands J Med Chem (2022) 65, 13013-13028. PubMed Europe PubMed DOI
Gackowski,M., Szewczyk-Golec,K., Madra-Gackowska,K., Pluskota,R. and Koba,M. Quantitative Structure-Activity Relationship Analysis of Isosteviol-Related Compounds as Activated Coagulation Factor X (FXa) Inhibitors Nutrients (2022) 14 PubMed Europe PubMed DOI
Modrzycka,S., Kolt,S., Polderdijk,S.G.I., Adams,T.E., Potoczek,S., Huntington,J.A., Kasperkiewicz,P. and Drag,M. Parallel imaging of coagulation pathway proteases activated protein C, thrombin, and factor Xa in human plasma Chem Sci (2022) 13, 6813-6829. PubMed Europe PubMed DOI PMC EPMC
Payne,J., Batsuli,G., Leavitt,A.D., Mathias,M. and McGuinn,C.E. A review of the pharmacokinetics, efficacy and safety of high-purity factor X for the prophylactic treatment of hereditary factor X deficiency Haemophilia (2022) 28, 523-531. PubMed Europe PubMed DOI
Ruben,E.A., Summers,B., Rau,M.J., Fitzpatrick,J.A.J. and Di Cera,E. Cryo-EM structure of the prothrombin-prothrombinase complex Blood (2022) 139, 3463-3473. PubMed Europe PubMed DOI PMC EPMC
Schroer,K., Alshawabkeh,M., Schellhorn,S., Bronder,K., Zhang,W. and Ehrhardt,A. Influence of Heparan Sulfate Proteoglycans and Factor X on species D Human Adenovirus Uptake and Transduction Viruses (2022) 15 PubMed Europe PubMed DOI PMC EPMC
Zekri-Nechar,K., Zamorano-Leon,J.J., Reche,C., Giner,M., Lopez-de-Andres,A., Jimenez-Garcia,R., Lopez-Farre,A.J. and Martinez-Martinez,C.H. Spike Protein Subunits of SARS-CoV-2 Alter Mitochondrial Metabolism in Human Pulmonary Microvascular Endothelial Cells: Involvement of Factor Xa Dis Markers (2022) 2022, 1118195-1118195. PubMed Europe PubMed DOI PMC EPMC
Zhang,Z.L., Chen,C., Qu,S.Y., Ding,Q. and Xu,Q. Unexpected Dynamic Binding May Rescue the Binding Affinity of Rivaroxaban in a Mutant of Coagulation Factor X Front Mol Biosci (2022) 9, 877170-877170. PubMed Europe PubMed DOI PMC EPMC I

2021

Ebert,M., Raquet,E., Schweisgut,S., Schmidt,P.M. and Weimer,T. Identification of a modified coagulation factor X with enhanced activation properties as potential hemostatic agent Blood Cells Mol Dis (2021) 89, 102570-102570. PubMed Europe PubMed DOI
Fischer,A., Sellner,M., Mitusinska,K., Bzowka,M., Lill,M.A., Gora,A. and Smiesko,M. Computational Selectivity Assessment of Protease Inhibitors against SARS-CoV-2 Int J Mol Sci (2021) 22 PubMed Europe PubMed DOI PMC EPMC
Ichinose,A., Osaki,T. and Souri,M. Autoimmune Coagulation Factor X Deficiency as a Rare Acquired Hemorrhagic Disorder: A Literature Review Thromb Haemost (2021) PubMed Europe PubMed DOI
Jackson,C.M. Structure and function of factor X: properties, activation, and activity in prothrombinase. A retrospective in a historical context J Thromb Thrombolysis (2021) PubMed Europe PubMed DOI
Kundu,S. and Wu,S. A Structure Based Study of Selective Inhibition of Factor IXa over Factor Xa Molecules (2021) 26 PubMed Europe PubMed DOI PMC EPMC
Paul,D. and Morrissey,J.H. Stoichiometric analysis reveals a unique phosphatidylserine binding site in coagulation factor X J Thromb Haemost (2021) PubMed Europe PubMed DOI
Ruf,W. Roles of factor Xa beyond coagulation J Thromb Thrombolysis (2021) PubMed Europe PubMed DOI

2020

Al-Horani,R.A. Potential Therapeutic Roles for Direct Factor Xa Inhibitors in Coronavirus Infections Am J Cardiovasc Drugs (2020) 20, 525-533. PubMed Europe PubMed DOI PMC EPMC V
Basavaraj,M.G. and Krishnaswamy,S. Exosite binding drives substrate affinity for the activation of coagulation factor X by the intrinsic Xase complex J Biol Chem (2020) PubMed Europe PubMed DOI
de Laat-Kremers,R.M.W., Yan,Q., Ninivaggi,M., de Maat,M. and de Laat,B. Deciphering the coagulation profile through the dynamics of thrombin activity Sci Rep (2020) 10, 12544-12544. PubMed Europe PubMed DOI PMC EPMC
Dorgalaleh,A., Baghaipour,M.R., Tabibian,S., Ghazizadeh,F., Dabbagh,A., Bahoush,G., Jazebi,M., Bahraini,M., Fazeli,A., Baghaipour,N. and Yousefi,F. Gastrointestinal bleeding in a newborn infant with congenital factor X deficiency and COVID-19-A common clinical feature between a rare disorder and a new, common infection Int J Lab Hematol (2020) PubMed Europe PubMed DOI PMC EPMC
Frydman,G.H., Streiff,M.B., Connors,J.M. and Piazza,G. The Potential Role of Coagulation Factor Xa in the Pathophysiology of COVID-19: A Role for Anticoagulants as Multimodal Therapeutic Agents TH Open (2020) 4, e288-e288. PubMed Europe PubMed DOI PMC EPMC V
Papadaki,S., Sidiropoulou,S., Moschonas,I.C. and Tselepis,A.D. Factor Xa and thrombin induce endothelial progenitor cell activation. The effect of direct oral anticoagulants Platelets (2020) , 1-8. PubMed Europe PubMed DOI I
Ruf,W. and Graf,C. Coagulation signaling and cancer immunotherapy Thromb Res (2020) 191 Suppl 1, S106-S106. PubMed Europe PubMed DOI
Shima,M. Bispecific Antibodies and Advances in Non-Gene Therapy Options in Hemophilia Res Pract Thromb Haemost (2020) 4, 446-454. PubMed Europe PubMed DOI PMC EPMC
Stallone,G., Pontrelli,P., Rascio,F., Castellano,G., Gesualdo,L. and Grandaliano,G. Coagulation and Fibrinolysis in Kidney Graft Rejection Front Immunol (2020) 11, 1807-1807. PubMed Europe PubMed DOI PMC EPMC V
Zhang,X., Chen,K., Wang,G., Zhang,C., Zhao,B., Liu,X., Qin,X. and Yang,L. Molecular mechanism of a novel Ser362Asn mutation causing inherited FX deficiency in a Chinese family Int J Hematol (2020) 112, 8-16. PubMed Europe PubMed DOI M
Zimowski,K.L., McGuinn,C.E., Abajas,Y.L., Schultz,C.L., Kaicker,S. and Batsuli,G. Use of plasma-derived factor X concentrate in neonates and infants with congenital factor X deficiency J Thromb Haemost (2020) 18, 2551-2556. PubMed Europe PubMed DOI

2019

Abache,T., Fontayne,A., Grenier,D., Jacque,E., Longue,A., Dezetter,A.S., Souilliart,B., Chevreux,G., Bataille,D., Chtourou,S. and Plantier,J.L. A mutated factor X activatable by thrombin corrects bleedings in vivo in a rabbit model of antibody-induced hemophilia A Haematologica (2019) 105, 2335-2340. PubMed Europe PubMed DOI
Ferrarese,M., Pignani,S., Lombardi,S., Balestra,D., Bernardi,F., Pinotti,M. and Branchini,A. The carboxyl-terminal region of human coagulation factor X as a natural linker for fusion strategies Thromb Res (2019) 173, 4-11. PubMed Europe PubMed DOI E
Ferrarese,M., Baroni,M., Della Valle,P., Spiga,I., Poloniato,A., D'Angelo,A., Pinotti,M., Bernardi,F. and Branchini,A. Missense changes in the catalytic domain of coagulation factor X account for minimal function preventing a perinatal lethal condition Haemophilia (2019) 25, 685-692. PubMed Europe PubMed DOI M
Girard,T.J., Lasky,N.M., Grunz,K. and Broze GJ Jr Suppressing protein Z-dependent inhibition of factor Xa improves coagulation in hemophilia A J Thromb Haemost (2019) 17, 149-156. PubMed Europe PubMed DOI
Girolami,A., de Paoletti,D.N.G., Nenkies,M.L., Ferrari,S. and Guglielmone,H. Factor X deficiency due to a compound heterozygosis between a new mutation (Gla72Asp) in exon 2 and an already known one (Gly154Arg) in exon 5: factor X Mar del Plata1) Cardiovasc Hematol Disord Drug Targets (2019) 19, 169-173. PubMed Europe PubMed DOI M
Ilin,I., Lipets,E., Sulimov,A., Kutov,D., Shikhaliev,K., Potapov,A., Krysin,M., Zubkov,F., Sapronova,L., Ataullakhanov,F. and Sulimov,V. New factor Xa inhibitors based on 1,2,3,4-tetrahydroquinoline developed by molecular modelling J Mol Graph Model (2019) 89, 215-224. PubMed Europe PubMed DOI I
Li,F., Chen,C., Qu,S.Y., Zhao,M.Z., Xie,X., Wu,X., Li,L., Wang,X., Ding,Q., Xu,Q., Wei,D.Q. and Wu,W. The disulfide bond between Cys22 and Cys27 in the protease domain modulate clotting activity of coagulation factor X Thromb Haemost (2019) 119, 871-881. PubMed Europe PubMed DOI
Mitchell,M., Gattens,M., Kavakli,K., Liesner,R., Payne,J., Norton,M. and Austin,S. Genotype analysis and identification of novel mutations in a multicentre cohort of patients with hereditary factor X deficiency Blood Coagul Fibrinolysis (2019) 30, 34-41. PubMed Europe PubMed DOI M
Muczynski,V., Verhenne,S., Casari,C., Cherel,G., Panicot-Dubois,L., Gueguen,P., Trossaert,M., Dubois,C., Lenting,P.J., Denis,C.V. and Christophe,O.D. A thrombin-activatable factor X variant corrects hemostasis in a mouse model for hemophilia A Thromb Haemost (2019) 119, 1981-1993. PubMed Europe PubMed DOI U
Othman,T., Abdelkarim,A., Huynh,K., Uche,A. and Lee,J. Inherited moderate factor X deficiency presenting as cardiac tamponade Case Rep Hematol (2019) 2019, 9657516-9657516. PubMed Europe PubMed DOI PMC EPMC M
Qu,S.Y., Xu,Q., Wu,W., Li,F., Li,C.D., Huang,R., Ding,Q. and Wei,D.Q. An unexpected dynamic binding mode between coagulation factor X and rivaroxaban reveals importance of flexibility in drug binding Chem Biol Drug Des (2019) 94, 1664-1671. PubMed Europe PubMed DOI I
van Dievoet,M.A., Jacquemin,M., Van Calsteren,K. and Peerlinck,K. A rare presentation of homozygous factor X deficiency in a pregnant patient: a case report and review of the literature Haemophilia (2019) 25, e57-e57. PubMed Europe PubMed DOI M

2018

Arita,K., Niimi,H., Yamagishi,N., Ueno,T., Kitajima,I. and Sugiyama,T. Factor X heterozygous mutation in a patient with potential risk of bleeding: a case report Medicine (Baltimore) (2018) 97, e10950-e10950. PubMed Europe PubMed DOI M
Augustsson,C., Svensson,A., Kjaer,B., Chao,T.Y., Wenjuan,X., Krogh,B.O., Breinholt,J., Clausen,J.T., Hilden,I., Petersen,H.H. and Petersen,L.C. Factor Xa and VIIa inhibition by tissue factor pathway Inhibitor is prevented by a monoclonal antibody to its Kunitz-1 domain J Thromb Haemost (2018) 16, 893-904. PubMed Europe PubMed DOI
Girolami,A., Cosi,E., Santarossa,C., Ferrari,S., Girolami,B. and Lombardi,A.M. Factor X Friuli coagulation disorder: almost 50 years later Clin Appl Thromb Hemost (2018) 24, 33-40. PubMed Europe PubMed DOI M
Gunaratne,R., Kumar,S., Frederiksen,J.W., Stayrook,S., Lohrmann,J.L., Perry,K., Bompiani,K.M., Chabata,C.V., Thalji,N.K., Ho,M.D., Arepally,G., Camire,R.M., Krishnaswamy,S. and Sullenger,B.A. Combination of aptamer and drug for reversible anticoagulation in cardiopulmonary bypass Nat Biotechnol (2018) 36, 606-613. PubMed Europe PubMed DOI PMC EPMC
Horinaka,S., Sugawara,R., Yonezawa,Y. and Ishimitsu,T. Factor Xa inhibition by rivaroxaban in the trough steady state can significantly reduce thrombin generation Br J Clin Pharmacol (2018) 84, 79-87. PubMed Europe PubMed DOI I
Hu,X., Xiao,Y., Yu,C., Zuo,Y., Yang,W., Wang,X., Gu,B. and Li,J. Characterization of a novel selective factor Xa inhibitor, DJT06001, which reduces thrombus formation with low risk of bleeding Eur J Pharmacol (2018) 825, 85-91. PubMed Europe PubMed DOI I
Jourdi,G., Gouin-Thibault,I., Siguret,V., Gandrille,S., Gaussem,P. and Le Bonniec,B. FXa-alpha2-Macroglobulin complex neutralizes direct oral anticoagulants targeting FXa in vitro and in vivo Thromb Haemost (2018) 118, 1535-1544. PubMed Europe PubMed DOI U
Kanade,G.D., Pingale,K.D. and Karpe,Y.A. Activities of thrombin and factor Xa are essential for replication of hepatitis E virus and are possibly implicated in the ORF1 polyprotein processing J Virol (2018) 92, e01853-17-e01853-17. PubMed Europe PubMed DOI
Lu,G., Pine,P., Leeds,J.M., DeGuzman,F., Pratikhya,P., Lin,J., Malinowski,J., Hollenbach,S.J., Curnutte,J.T. and Conley,P.B. Andexanet alfa effectively reverses edoxaban anticoagulation effects and associated bleeding in a rabbit acute hemorrhage model PLoS ONE (2018) 13, e0195122-e0195122. PubMed Europe PubMed DOI I
Ramesh,K., Lama,D., Tan,K.W., Nguyen,V.S., Chew,F.T., Verma,C.S. and Mok,Y.K. Homologous lympho-epithelial Kazal-type inhibitor domains delay blood coagulation by inhibiting factor X and XI with differential specificity Structure (2018) 26, 1178-1186. PubMed Europe PubMed DOI
Shinozawa,E., Nakayama,M. and Imura,Y. TAK-442, a direct factor Xa inhibitor, inhibits monocyte chemoattractant protein 1 production in endothelial cells via involvement of protease-activated receptor 1 Front Pharmacol (2018) 9, 1431-1431. PubMed Europe PubMed DOI PMC EPMC I

2017

Hack,K., Renzi,F., Hess,E., Lauber,F., Douxfils,J., Dogne,J.M. and Cornelis,G.R. Inactivation of human coagulation factor X by a protease of the pathogen Capnocytophaga canimorsus J Thromb Haemost (2017) 15, 487-499. PubMed Europe PubMed DOI
Hu,Z., Liu,Y., Huarng,M.C., Menegatti,M., Reyon,D., Rost,M.S., Norris,Z.G., Richter,C.E., Stapleton,A.N., Chi,N.C., Peyvandi,F., Joung,J.K. and Shavit,J.A. Genome editing of factor X in zebrafish reveals unexpected tolerance of severe defects in the common pathway Blood (2017) 130, 666-676. PubMed Europe PubMed DOI
Jaegle,M., Steinmetzer,T. and Rademann,J. Protein-templated formation of an inhibitor of the blood coagulation factor Xa through a background-free amidation reaction Angew Chem Int Ed Engl (2017) 56, 3718-3722. PubMed Europe PubMed DOI I
Kovalenko,T.A., Panteleev,M.A. and Sveshnikova,A.N. Substrate delivery mechanism and the role of membrane curvature in factor X activation by extrinsic tenase J Theor Biol (2017) 435, 125-133. PubMed Europe PubMed DOI
Lagos,C.F., Segovia,G.F., Nunez-Navarro,N., Faundez,M.A. and Zacconi,F.C. Novel FXa inhibitor identification through integration of ligand- and structure-based approaches Molecules (2017) 22 PubMed Europe PubMed DOI I
Lenting,P.J., Denis,C.V. and Christophe,O.D. Emicizumab, a bispecific antibody recognizing coagulation factors IX and X: how does it actually compare to factor VIII? Blood (2017) 130, 2463-2468. PubMed Europe PubMed DOI
Thalji,N.K. and Camire,R.M. Rendering factor Xa zymogen-like as a therapeutic strategy to treat bleeding Curr Opin Hematol (2017) 24, 453-459. PubMed Europe PubMed DOI U

2016

Arian,D., Harenberg,J. and Kramer,R. A chromogenic and fluorogenic peptide substrate for the highly sensitive detection of proteases in biological matrices J Med Chem (2016) 59, 7576-7583. PubMed Europe PubMed DOI A
Camire,R.M. Bioengineering factor Xa to treat bleeding Thromb Res (2016) 141 Suppl 2, S31-S33. PubMed Europe PubMed DOI E U
Escobar,M.A., Auerswald,G., Austin,S., Huang,J.N., Norton,M. and Millar,C.M. Experience of a new high-purity factor X concentrate in subjects with hereditary factor X deficiency undergoing surgery Haemophilia (2016) 22, 713-720. PubMed Europe PubMed DOI U
Girish,V.M. and Kini,R.M. Exactin: a specific inhibitor of factor X activation by extrinsic tenase complex from the venom of Hemachatus haemachatus Sci Rep (2016) 6, 32036-32036. PubMed Europe PubMed DOI PMC EPMC
Girolami,A., Molina,M.A., Galletti,M.L., Ferrari,S., Sambado,L. and Guglielmone,H. A family with factor X deficiency from Argentina: a compound heterozygosis because of the combination of a new mutation (Gln138Arg) with an already known one (Glu350Lys) Blood Coagul Fibrinolysis (2016) 27, 732-736. PubMed Europe PubMed DOI M
Peraramelli,S., Thomassen,S., Heinzmann,A., Hackeng,T.M., Hartmann,R., Scheiflinger,F., Dockal,M. and Rosing,J. Role of exosite binding modulators in the inhibition of FXa by TFPI Thromb Haemost (2016) 115, 580-590. PubMed Europe PubMed DOI
Pryzdial,E.L., Meixner,S.C., Talbot,K., Eltringham-Smith,L.J., Baylis,J.R., Lee,F.M., Kastrup,C.J. and Sheffield,W.P. Thrombolysis by chemically modified coagulation factor Xa J Thromb Haemost (2016) 14, 1844-1854. PubMed Europe PubMed DOI
Sharma,M., Iyer,J.K., Shih,N., Majumder,M., Mattaparthi,V.S., Mukhopadhyay,R. and Doley,R. Daboxin P, a major phospholipase A2 enzyme from the Indian Daboia russelii russelii venom targets factor X and factor Xa for its anticoagulant activity PLoS ONE (2016) 11, e0153770-e0153770. PubMed Europe PubMed DOI
Sun,N., Chen,Y., Peng,H., Luo,Y. and Zhang,G. A novel Ala275Val mutation in factor X gene influences its structural compatibility and impairs intracellular trafficking and coagulant activity Thromb Res (2016) 138, 108-113. PubMed Europe PubMed DOI M

2015

Baroni,M., Pavani,G., Pinotti,M., Branchini,A., Bernardi,F. and Camire,R.M. Asymmetric processing of mutant factor X Arg386Cys reveals differences between intrinsic and extrinsic pathway activation Biochim Biophys Acta (2015) 1854, 1351-1356. PubMed Europe PubMed DOI
Block,H., Maertens,B., Spriestersbach,A., Kubicek,J. and Schafer,F. Proteolytic affinity tag cleavage Methods Enzymol (2015) 559, 71-97. PubMed Europe PubMed DOI
Branchini,A., Baroni,M., Burini,F., Puzzo,F., Nicolosi,F., Mari,R., Gemmati,D., Bernardi,F. and Pinotti,M. The carboxyl-terminal region is NOT essential for secreted and functional levels of coagulation factor X J Thromb Haemost (2015) 13, 1468-1474. PubMed Europe PubMed DOI
Chevreux,G., Tilly,N., Faid,V. and Bihoreau,N. Mass spectrometry based analysis of human plasma-derived factor X revealed novel post-translational modifications Protein Sci (2015) 24, 1640-1648. PubMed Europe PubMed DOI
Corsini,I., Menegatti,M., Cairo,A. and Dani,C. Neonatal onset of congenital factor X deficiency: a description of two novel mutations with 6-year follow-up Blood Coagul Fibrinolysis (2015) 26, 679-681. PubMed Europe PubMed DOI M
Eyre,T.A., Bignell,P. and Keeling,D. Factor X deficiency associated with compound heterozygosity involving a novel missense mutation at codon 38 from Val (GTC) to Leu (CTC) in exon 2 Blood Coagul Fibrinolysis (2015) 26, 352-353. PubMed Europe PubMed DOI M
Girolami,A., Cosi,E., Sambado,L., Girolami,B. and Randi,M.L. Complex history of the discovery and characterization of congenital factor X deficiency Semin Thromb Hemost (2015) 41, 359-365. PubMed Europe PubMed DOI V
Ivanciu,L. and Camire,R.M. Hemostatic agents of broad applicability produced by selective tuning of factor Xa zymogenicity Blood (2015) 126, 94-102. PubMed Europe PubMed DOI U
Noguchi,K., Morishima,Y., Takahashi,S., Ishihara,H., Shibano,T. and Murata,M. Impact of nonsynonymous mutations of factor X on the functions of factor X and anticoagulant activity of edoxaban Blood Coagul Fibrinolysis (2015) 26, 117-122. PubMed Europe PubMed DOI M I
Wang,Y., Ma,J., Liu,X., Wang,Y., Wang,H., Wang,L., Ding,Q., Chu,X. and Hou,M. A novel factor X gene mutation Val (GTC) 384Ala (GCC) in a Chinese family resulting in congenital factor X deficiency Int J Clin Exp Med (2015) 8, 10095-10098. PubMed Europe PubMed PMC EPMC M

2014

Abdel-Azeim,S., Oliva,R., Chermak,E., De Cristofaro,R. and Cavallo,L. Molecular dynamics characterization of five pathogenic factor X mutants associated with decreased catalytic activity Biochemistry (2014) 53, 6992-7001. PubMed Europe PubMed DOI M
Belviso,B.D., Caliandro,R., de Candia,M., Zaetta,G., Lopopolo,G., Incampo,F., Colucci,M. and Altomare,C.D. How a beta-D-glucoside side chain enhances binding affinity to thrombin of inhibitors bearing 2-chlorothiophene as P1 moiety: crystallography, fragment deconstruction study, and evaluation of antithrombotic properties J Med Chem (2014) 57, 8563-8575. PubMed Europe PubMed DOI I
Bijak,M., Ponczek,M.B. and Nowak,P. Polyphenol compounds belonging to flavonoids inhibit activity of coagulation factor X Int J Biol Macromol (2014) 65, 129-135. PubMed Europe PubMed DOI I
Bounameaux,H. and Camm,A.J. Edoxaban: an update on the new oral direct factor Xa inhibitor Drugs (2014) 74, 1209-1231. PubMed Europe PubMed DOI I
Chikasawa,Y., Shinozawa,K., Amano,K., Ogata,K., Hagiwara,T., Suzuki,T., Inaba,H. and Fukutake,K. Factor X M402T: a homozygous missense mutation identified as the cause of cross-reacting material-reduced deficiency Int J Hematol (2014) 100, 345-352. PubMed Europe PubMed DOI M
Esmon,C.T. Targeting factor Xa and thrombin: impact on coagulation and beyond Thromb Haemost (2014) 111, 625-633. PubMed Europe PubMed DOI I
Jiang,L., Wang,Q., Shen,S., Xiao,T. and Li,Y. Discovery of glycyrrhetinic acid as an orally active, direct inhibitor of blood coagulation factor Xa Thromb Res (2014) 133, 501-506. PubMed Europe PubMed DOI I
Lu,Q., Yang,L., Manithody,C., Wang,X. and Rezaie,A.R. Molecular basis of the clotting defect in a bleeding patient missing the Asp-185 codon in the factor X gene Thromb Res (2014) 134, 1103-1109. PubMed Europe PubMed DOI M
Menegatti,M., Vangone,A., Palla,R., Milano,G., Cavallo,L., Oliva,R., De Cristofaro,R. and Peyvandi,F. A recurrent Gly43Asp substitution in coagulation factor X rigidifies its catalytic pocket and impairs catalytic activity and intracellular trafficking Thromb Res (2014) 133, 481-487. PubMed Europe PubMed DOI M
Mourier,P.A., Guichard,O.Y., Herman,F. and Viskov,C. Isolation of a pure octadecasaccharide with antithrombin activity from an ultra-low-molecular-weight heparin Anal Biochem (2014) 453, 7-15. PubMed Europe PubMed DOI
Nguyen,C.N., Cruz,A., Gilson,M.K. and Kurtzman,T. Thermodynamics of water in an enzyme active site: grid-based hydration analysis of coagulation factor Xa J Chem Theory Comput (2014) 10, 2769-2780. PubMed Europe PubMed DOI PMC EPMC
Pomowski,A., Ustok,F.I. and Huntington,J.A. Homology model of human prothrombinase based on the crystal structure of pseutarin C Biol Chem (2014) 395, 1233-1241. PubMed Europe PubMed DOI
Pozzi,N., Chen,Z., Pelc,L.A., Shropshire,D.B. and Di Cera,E. The linker connecting the two kringles plays a key role in prothrombin activation Proc Natl Acad Sci U S A (2014) 111, 7630-7635. PubMed Europe PubMed DOI
Thakur,R., Kumar,A., Bose,B., Panda,D., Saikia,D., Chattopadhyay,P. and Mukherjee,A.K. A new peptide (Ruviprase) purified from the venom of Daboia russelii russelii shows potent anticoagulant activity via non-enzymatic inhibition of thrombin and factor Xa Biochimie (2014) 105, 149-158. PubMed Europe PubMed DOI I

2013

Ding,Q., Shen,Y., Yang,L., Wang,X. and Rezaie,A.R. The missense Thr211Pro mutation in the factor X activation peptide of a bleeding patient causes molecular defect in the clotting cascade Thromb Haemost (2013) 110, 53-61. PubMed Europe PubMed DOI M
Griffiths,A.E., Wintermute,J., Newell-Caito,J.L. and Fay,P.J. Residues flanking scissile bonds in factor VIII modulate rates of cleavage and proteolytic activation catalyzed by factor Xa Biochemistry (2013) 52, 8060-8068. PubMed Europe PubMed DOI P
King,C.S., Holley,A.B. and Moores,L.K. Moving toward a more ideal anticoagulant: the oral direct thrombin and factor Xa inhibitors Chest (2013) 143, 1106-1116. PubMed Europe PubMed DOI I
Lu,G., Deguzman,F.R., Hollenbach,S.J., Karbarz,M.J., Abe,K., Lee,G., Luan,P., Hutchaleelaha,A., Inagaki,M., Conley,P.B., Phillips,D.R. and Sinha,U. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa Nat Med (2013) 19, 446-451. PubMed Europe PubMed DOI
Meneyrol,J., Follmann,M., Lassalle,G., Wehner,V., Barre,G., Rousseaux,T., Altenburger,J.M., Petit,F., Bocskei,Z., Schreuder,H., Alet,N., Herault,J.P., Millet,L., Dol,F., Florian,P., Schaeffer,P., Sadoun,F., Klieber,S., Briot,C., Bono,F. and Herbert,J.M. 5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor J Med Chem (2013) 56, 9441-9456. PubMed Europe PubMed DOI I
Talbot,K., Meixner,S.C. and Pryzdial,E.L. Proteolytic modulation of factor Xa-antithrombin complex enhances fibrinolysis in plasma Biochim Biophys Acta (2013) 1834, 989-995. PubMed Europe PubMed DOI
Zhou,J.W., Liang,Q., Chen,Q., Xie,Y., Ding,Q.L., Wang,X.F., Xi,X.D. and Wang,H.L. Molecular defects in the factor X gene caused by novel heterozygous mutations IVS5+1G>A and Asp409del Haemophilia (2013) 19, 94-99. PubMed Europe PubMed DOI M

2012

Ahrens,I. and Bode,C. New parenteral anticoagulants: focus on factor Xa and thrombin inhibitors Curr Drug Discov Technol (2012) 9, 129-136. PubMed Europe PubMed I
Becattini,C., Lignani,A. and Agnelli,G. New oral anticoagulants for venous thromboembolism: focus on factor Xa and thrombin inhibitors Curr Drug Discov Technol (2012) 9, 119-128. PubMed Europe PubMed I
Brown,M.A., Stenberg,L.M. and Stenflo,J. Coagulation factor Xa [ISSN:978-0-12-407742-3] (2012) 3, 2908-2915. DOI
Lopopolo,G., de Candia,M., Panza,L., Romano,M.R., Lograno,M.D., Campagna,F. and Altomare,C. beta-D-Glucosyl conjugates of highly potent inhibitors of blood coagulation factor Xa bearing 2-chorothiophene as a P1 motif ChemMedChem (2012) 7, 1669-1677. PubMed Europe PubMed DOI I
Marlu,R. and Polack,B. Gla-domainless factor Xa: molecular bait to bypass a blocked tenase complex Haematologica (2012) 97, 1165-1172. PubMed Europe PubMed DOI U
Nakatomi,Y., Tsuji,M., Gokudan,S., Hanada-Dateki,T., Nakashima,T., Miyazaki,H., Hamamoto,T., Nakagaki,T. and Tomokiyo,K. Stable complex formation between serine protease inhibitor and zymogen: coagulation factor X cleaves the Arg393-Ser394 bond in a reactive centre loop of antithrombin in the presence of heparin J Biochem (2012) 152, 463-470. PubMed Europe PubMed DOI P
Nar,H. The role of structural information in the discovery of direct thrombin and factor Xa inhibitors Trends Pharmacol Sci (2012) 33, 279-288. PubMed Europe PubMed DOI V I
Olson,S.T., Swanson,R. and Petitou,M. Specificity and selectivity profile of EP217609: a new neutralizable dual-action anticoagulant that targets thrombin and factor Xa Blood (2012) 119, 2187-2195. PubMed Europe PubMed DOI I
Salonen,L.M., Holland,M.C., Kaib,P.S., Haap,W., Benz,J., Mary,J.L., Kuster,O., Schweizer,W.B., Banner,D.W. and Diederich,F. Molecular recognition at the active site of factor Xa: cation-pi interactions, stacking on planar peptide surfaces, and replacement of structural water Chemistry (2012) 18, 213-222. PubMed Europe PubMed DOI
Takeyama,M., Wakabayashi,H. and Fay,P.J. Factor VIII light chain contains a binding site for factor X that contributes to the catalytic efficiency of factor Xase Biochemistry (2012) 51, 820-828. PubMed Europe PubMed DOI
Vanden Hoek,A.L., Talbot,K., Carter,I.S., Vickars,L., Carter,C.J., Jackson,S.C., MacGillivray,R.T. and Pryzdial,E.L. Coagulation factor X Arg386 specifically affects activation by the intrinsic pathway: a novel patient mutation J Thromb Haemost (2012) 10, 2613-2615. PubMed Europe PubMed DOI M

2011

Bhunia,S.S., Roy,K.K. and Saxena,A.K. Profiling the structural determinants for the selectivity of representative factor-Xa and thrombin inhibitors using combined ligand-based and structure-based approaches J Chem Inf Model (2011) 51, 1966-1985. PubMed Europe PubMed DOI I
Bunce,M.W., Toso,R. and Camire,R.M. Zymogen-like factor Xa variants restore thrombin generation and effectively bypass the intrinsic pathway in vitro Blood (2011) 117, 290-298. PubMed Europe PubMed DOI U
Duffy,M.R., Bradshaw,A.C., Parker,A.L., McVey,J.H. and Baker,A.H. A cluster of basic amino acids in the factor X serine protease mediates surface attachment of adenovirus/FX complexes J Virol (2011) 85, 10914-10919. PubMed Europe PubMed DOI
Hirayama,F., Koshio,H., Ishihara,T., Hachiya,S., Sugasawa,K., Koga,Y., Seki,N., Shiraki,R., Shigenaga,T., Iwatsuki,Y., Moritani,Y., Mori,K., Kadokura,T., Kawasaki,T., Matsumoto,Y., Sakamoto,S. and Tsukamoto,S. Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide (Darexaban, YM150) as a potent and orally available factor Xa inhibitor J Med Chem (2011) 54, 8051-8065. PubMed Europe PubMed DOI I
Ivanciu,L., Toso,R., Margaritis,P., Pavani,G., Kim,H., Schlachterman,A., Liu,J.H., Clerin,V., Pittman,D.D., Rose-Miranda,R., Shields,K.M., Erbe,D.V., Tobin,J.F., Arruda,V.R. and Camire,R.M. A zymogen-like factor Xa variant corrects the coagulation defect in hemophilia Nat Biotechnol (2011) 29, 1028-1033. PubMed Europe PubMed DOI
Livnat,T., Shenkman,B., Kenet,G., Tamarin,I., Gillis,S., Varon,D., Iijima,K., Zivelin,A. and Salomon,O. Severe factor X deficiency in three unrelated Palestinian patients is caused by homozygosity for the mutation c302delG - correlation with thrombin generation and thromboelastometry Blood Coagul Fibrinolysis (2011) 22, 673-679. PubMed Europe PubMed DOI M
Lopopolo,G., Fiorella,F., de Candia,M., Nicolotti,O., Martel,S., Carrupt,P.A. and Altomare,C. Biarylmethoxy isonipecotanilides as potent and selective inhibitors of blood coagulation factor Xa Eur J Pharm Sci (2011) 42, 180-191. PubMed Europe PubMed DOI I
Schilling,O., dem Keller,U.A. and Overall,C.M. Factor Xa subsite mapping by proteome-derived peptide libraries improved using WebPICS, a resource for proteomic identification of cleavage sites Biol Chem (2011) 392, 1031-1037. PubMed Europe PubMed DOI P
Siigur,J. and Siigur,E. Activation of factor X by snake venom proteases (2011) , 447-464. DOI
Straub,A., Roehrig,S. and Hillisch,A. Oral, direct thrombin and factor Xa inhibitors: the replacement for warfarin, leeches, and pig intestines? Angew Chem Int Ed Engl (2011) 50, 4574-4590. PubMed Europe PubMed DOI I

2010

Barone,A., Campbell,J., Griffin,G. and Hill,M. Factor X Umuahia: a severe bleeding diathesis associated with a novel mutation Pediatr Blood Cancer (2010) 55, 1246-1246. PubMed Europe PubMed DOI M
Borensztajn,K., Peppelenbosch,M.P. and Spek,C.A. Coagulation factor Xa inhibits cancer cell migration via LIMK1-mediated cofilin inactivation Thromb Res (2010) 125, e323-e328. PubMed Europe PubMed DOI
Gueguen,P., Cherel,G., Badirou,I., Denis,C.V. and Christophe,O.D. Two residues in the activation peptide domain contribute to the half-life of factor X in vivo J Thromb Haemost (2010) 8, 1651-1653. PubMed Europe PubMed DOI
Huang,X., Dementiev,A., Olson,S.T. and Gettins,P.G. Basis for the specificity and activation of the serpin protein Z-dependent proteinase inhibitor (ZPI) as an inhibitor of membrane-associated factor Xa J Biol Chem (2010) 285, 20399-20409. PubMed Europe PubMed DOI
Lee,C.J., Chandrasekaran,V., Wu,S., Duke,R.E. and Pedersen,L.G. Recent estimates of the structure of the factor VIIa (FVIIa)/tissue factor (TF) and factor Xa (FXa) ternary complex Thromb Res (2010) 125 Suppl 1, S7-S7. PubMed Europe PubMed DOI S
Talbot,K., Meixner,S.C. and Pryzdial,E.L. Enhanced fibrinolysis by proteolysed coagulation factor Xa Biochim Biophys Acta (2010) 1804, 723-730. PubMed Europe PubMed DOI
Wallnoefer,H.G., Handschuh,S., Liedl,K.R. and Fox,T. Stabilizing of a globular protein by a highly complex water network: a molecular dynamics simulation study on factor Xa J Phys Chem B (2010) 114, 7405-7412. PubMed Europe PubMed DOI S

2009

Borensztajn,K., Bijlsma,M.F., Reitsma,P.H., Peppelenbosch,M.P. and Spek,C.A. Coagulation factor Xa inhibits cancer cell migration via protease-activated receptor-1 activation Thromb Res (2009) 124, 219-225. PubMed Europe PubMed DOI U
Chafa,O., Tagzirt,M., Tapon-Bretaudiere,J., Reghis,A., Fischer,A.M. and LeBonniec,B.F. Characterization of a homozygous Gly11Val mutation in the Gla domain of coagulation factor X Thromb Res (2009) 124, 144-148. PubMed Europe PubMed DOI M
Chen,Y., Qin,S., Tan,W., Lu,Y., Zhang,J., Li,H., Bu,H. and Cheng,J. Cloning and comparison of factor X from rhesus monkey (Macaca mulatta) Comp Med (2009) 59, 476-481. PubMed Europe PubMed PMC EPMC
Glauser,B.F., Rezende,R.M., Melo,F.R., Pereira,M.S., Francischetti,I.M., Monteiro,R.Q., Rezaie,A.R. and Mourao,P.A. Anticoagulant activity of a sulfated galactan: serpin-independent effect and specific interaction with factor Xa Thromb Haemost (2009) 102, 1183-1193. PubMed Europe PubMed DOI PMC EPMC
Menegatti,M. and Peyvandi,F. Factor X deficiency Semin Thromb Hemost (2009) 35, 407-415. PubMed Europe PubMed DOI M
Monti,M., Borensztajn,K.S., Pinotti,M., Canella,A., Branchini,A., Marchetti,G., Reitsma,P.H., Bernardi,F. and Spek,C.A. Characterization of the intracellular signalling capacity of natural FXa mutants with reduced pro-coagulant activity Thromb Res (2009) 123, 914-918. PubMed Europe PubMed DOI
Rosborough,T.K., Jacobsen,J.M. and Shepherd,M.F. Relationship between chromogenic factor X and international normalized ratio differs during early warfarin initiation compared with chronic warfarin administration Blood Coagul Fibrinolysis (2009) 20, 433-435. PubMed Europe PubMed DOI A
Salonen,L.M., Bucher,C., Banner,D.W., Haap,W., Mary,J.L., Benz,J., Kuster,O., Seiler,P., Schweizer,W.B. and Diederich,F. Cation-pi interactions at the active site of factor Xa: dramatic enhancement upon stepwise N-alkylation of ammonium ions Angew Chem Int Ed Engl (2009) 48, 811-814. PubMed Europe PubMed DOI
Van Huis,C.A., Casimiro-Garcia,A., Bigge,C.F., Cody,W.L., Dudley,D.A., Filipski,K.J., Heemstra,R.J., Kohrt,J.T., Leadley,R.J., Jr., Narasimhan,L.S., McClanahan,T., Mochalkin,I., Pamment,M., Peterson,J.T., Sahasrabudhe,V., Schaum,R.P. and Edmunds,J.J. Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active factor Xa inhibitors with extended duration of action Bioorg Med Chem (2009) 17, 2501-2511. PubMed Europe PubMed DOI I
Verghese,J., Liang,A., Sidhu,P.P., Hindle,M., Zhou,Q. and Desai,U.R. First steps in the direction of synthetic, allosteric, direct inhibitors of thrombin and factor Xa Bioorg Med Chem Lett (2009) 19, 4126-4129. PubMed Europe PubMed DOI PMC EPMC I
Wong,P.C., Crain,E.J., Watson,C.A. and Xin,B. Favorable therapeutic index of the direct factor Xa inhibitors, apixaban and rivaroxaban, compared with the thrombin inhibitor dabigatran in rabbits J Thromb Haemost (2009) 7, 1313-1320. PubMed Europe PubMed DOI I
Zikria,J.C. and Ansell,J. Oral anticoagulation with factor Xa and thrombin inhibitors: on the threshold of change Curr Opin Hematol (2009) 16, 347-356. PubMed Europe PubMed DOI I

2008

Abboud,M.A., Needle,S.J., Burns-Kurtis,C.L., Valocik,R.E., Koster,P.F., Amour,A.J., Chan,C., Brown,D., Chaudry,L., Zhou,P., Patikis,A., Patel,C., Pateman,A.J., Young,R.J., Watson,N.S. and Toomey,J.R. Antithrombotic potential of GW813893: a novel, orally active, active-site directed factor Xa inhibitor J Cardiovasc Pharmacol (2008) 52, 66-71. PubMed Europe PubMed DOI I
Bereczky,Z., Bardos,H., Komaromi,I., Kiss,C., Haramura,G., Ajzner,E., Adany,R. and Muszbek,L. Factor X Debrecen: Gly204Arg mutation in factor X causes the synthesis of a non-secretable protein and severe factor X deficiency Haematologica (2008) 93, 299-302. PubMed Europe PubMed DOI M
Brown,D.L. and Kouides,P.A. Diagnosis and treatment of inherited factor X deficiency Haemophilia (2008) 14, 1176-1182. PubMed Europe PubMed DOI M V
Chen,C.T., Yang,E.W., Hsu,H.J., Sun,Y.K., Hsu,W.L. and Yang,A.S. Protease substrate site predictors derived from machine learning on multilevel substrate phage display data Bioinformatics (2008) 24, 2691-2697. PubMed Europe PubMed DOI P
Corte,J.R., Fang,T., Pinto,D.J., Han,W., Hu,Z., Jiang,X.J., Li,Y.L., Gauuan,J.F., Hadden,M., Orton,D., Rendina,A.R., Luettgen,J.M., Wong,P.C., He,K., Morin,P.E., Chang,C.H., Cheney,D.L., Knabb,R.M., Wexler,R.R. and Lam,P.Y. Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties Bioorg Med Chem Lett (2008) 18, 2845-2849. PubMed Europe PubMed DOI I
Furugohri,T., Isobe,K., Honda,Y., Kamisato-Matsumoto,C., Sugiyama,N., Nagahara,T., Morishima,Y. and Shibano,T. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles J Thromb Haemost (2008) 6, 1542-1549. PubMed Europe PubMed DOI I
Hsu,H.J., Tsai,K.C., Sun,Y.K., Chang,H.J., Huang,Y.J., Yu,H.M., Lin,C.H., Mao,S.S. and Yang,A.S. Factor Xa active site substrate specificity with substrate phage display and computational molecular modeling J Biol Chem (2008) 283, 12343-12353. PubMed Europe PubMed DOI PMC EPMC P
Imaeda,Y., Miyawaki,T., Sakamoto,H., Itoh,F., Konishi,N., Hiroe,K., Kawamura,M., Tanaka,T. and Kubo,K. Discovery of sulfonylalkylamides: a new class of orally active factor Xa inhibitors Bioorg Med Chem (2008) 16, 2243-2260. PubMed Europe PubMed DOI I
Lee,Y.K., Parks,D.J., Lu,T., Thieu,T.V., Markotan,T., Pan,W., McComsey,D.F., Milkiewicz,K.L., Crysler,C.S., Ninan,N., Abad,M.C., Giardino,E.C., Maryanoff,B.E., Damiano,B.P. and Player,M.R. 7-fluoroindazoles as potent and selective inhibitors of factor Xa J Med Chem (2008) 51, 282-297. PubMed Europe PubMed DOI S I
Qiao,J.X., Cheney,D.L., Alexander,R.S., Smallwood,A.M., King,S.R., He,K., Rendina,A.R., Luettgen,J.M., Knabb,R.M., Wexler,R.R. and Lam,P.Y. Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa Bioorg Med Chem Lett (2008) 18, 4118-4123. PubMed Europe PubMed DOI S I
Shi,Y., Sitkoff,D., Zhang,J., Klei,H.E., Kish,K., Liu,E.C., Hartl,K.S., Seiler,S.M., Chang,M., Huang,C., Youssef,S., Steinbacher,T.E., Schumacher,W.A., Grazier,N., Pudzianowski,A., Apedo,A., Discenza,L., Yanchunas,J., Stein,P.D. and Atwal,K.S. Design, structure-activity relationships, X-ray crystal structure, and energetic contributions of a critical P1 pharmacophore: 3-chloroindole-7-yl-based factor Xa inhibitors J Med Chem (2008) 51, 7541-7551. PubMed Europe PubMed DOI S I
Smallheer,J.M., Wang,S., Laws,M.L., Nakajima,S., Hu,Z., Han,W., Jacobson,I., Luettgen,J.M., Rossi,K.A., Rendina,A.R., Knabb,R.M., Wexler,R.R., Lam,P.Y. and Quan,M.L. Sulfonamidolactam inhibitors of coagulation factor Xa Bioorg Med Chem Lett (2008) 18, 2428-2433. PubMed Europe PubMed DOI I
Tai,S.J., Herzog,R.W., Margaritis,P., Arruda,V.R., Chu,K., Golden,J.A., Labosky,P.A. and High,K.A. A viable mouse model of factor X deficiency provides evidence for maternal transfer of factor X J Thromb Haemost (2008) 6, 339-345. PubMed Europe PubMed DOI PMC EPMC K
Toso,R., Zhu,H. and Camire,R.M. The conformational switch from the factor X zymogen to protease state mediates exosite expression and prothrombinase assembly J Biol Chem (2008) 283, 18627-18635. PubMed Europe PubMed DOI PMC EPMC
Young,R.J., Borthwick,A.D., Brown,D., Burns-Kurtis,C.L., Campbell,M., Chan,C., Charbaut,M., Convery,M.A., Diallo,H., Hortense,E., Irving,W.R., Kelly,H.A., King,N.P., Kleanthous,S., Mason,A.M., Pateman,A.J., Patikis,A.N., Pinto,I.L., Pollard,D.R., Senger,S., Shah,G.P., Toomey,J.R., Watson,N.S., Weston,H.E. and Zhou,P. Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs Bioorg Med Chem Lett (2008) 18, 28-33. PubMed Europe PubMed DOI I
Young,R.J., Borthwick,A.D., Brown,D., Burns-Kurtis,C.L., Campbell,M., Chan,C., Charbaut,M., Chung,C.W., Convery,M.A., Kelly,H.A., Paul King,N., Kleanthous,S., Mason,A.M., Pateman,A.J., Patikis,A.N., Pinto,I.L., Pollard,D.R., Senger,S., Shah,G.P., Toomey,J.R., Watson,N.S. and Weston,H.E. Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs Bioorg Med Chem Lett (2008) 18, 23-27. PubMed Europe PubMed DOI I

2007

Ansell,J. Factor Xa or thrombin: is factor Xa a better target? J Thromb Haemost (2007) 5 Suppl 1, 60-64. PubMed Europe PubMed DOI V
Borensztajn,K.S., Bijlsma,M.F., Groot,A.P., Bruggemann,L.W., Versteeg,H.H., Reitsma,P.H., Peppelenbosch,M.P. and Spek,C.A. Coagulation factor Xa drives tumor cells into apoptosis through BH3-only protein Bim up-regulation Exp Cell Res (2007) 313, 2622-2633. PubMed Europe PubMed DOI
Chan,C., Borthwick,A.D., Brown,D., Burns-Kurtis,C.L., Campbell,M., Chaudry,L., Chung,C.W., Convery,M.A., Hamblin,J.N., Johnstone,L., Kelly,H.A., Kleanthous,S., Patikis,A., Patel,C., Pateman,A.J., Senger,S., Shah,G.P., Toomey,J.R., Watson,N.S., Weston,H.E., Whitworth,C., Young,R.J. and Zhou,P. Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides J Med Chem (2007) 50, 1546-1557. PubMed Europe PubMed DOI S I
Di Fenza,A., Heine,A., Koert,U. and Klebe,G. Understanding binding selectivity toward trypsin and factor Xa: the role of aromatic interactions ChemMedChem (2007) 2, 297-308. PubMed Europe PubMed DOI I
Donnecke,D., Schweinitz,A., Sturzebecher,A., Steinmetzer,P., Schuster,M., Sturzebecher,U., Nicklisch,S., Sturzebecher,J. and Steinmetzer,T. From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3 Bioorg Med Chem Lett (2007) 17, 3322-3329. PubMed Europe PubMed DOI I
Du,L., Kao,R.Y., Zhou,Y., He,Y., Zhao,G., Wong,C., Jiang,S., Yuen,K.Y., Jin,D.Y. and Zheng,B.J. Cleavage of spike protein of SARS coronavirus by protease factor Xa is associated with viral infectivity Biochem Biophys Res Commun (2007) 359, 174-179. PubMed Europe PubMed DOI PMC EPMC I
Franciskovich,J.B., Masters,J.J., Weber,W.W., Klimkowski,V.J., Chouinard,M., Sipes,P.R., Johnson,L.M., Snyder,D.W., Chastain,M.K., Craft,T.J., Towner,R.D., Gifford-Moore,D.S., Froelich,L.L., Smallwood,J.K., Foster,R.S., Smith,G.F., Liebeschuetz,J.W., Murray,C.W. and Young,S.C. Investigation of the terminal P4 domain in a series of d-phenylglycinamide-based factor Xa inhibitors Bioorg Med Chem Lett (2007) 17, 6910-6913. PubMed Europe PubMed DOI I
Gale,A.J., Yegneswaran,S., Xu,X., Pellequer,J.L. and Griffin,J.H. Characterization of a factor Xa binding site on factor Va near the Arg-506 activated protein C cleavage site J Biol Chem (2007) 282, 21848-21855. PubMed Europe PubMed DOI
Graff,J., von Hentig,N., Misselwitz,F., Kubitza,D., Becka,M., Breddin,H.K. and Harder,S. Effects of the oral, direct factor Xa inhibitor rivaroxaban on platelet-induced thrombin generation and prothrombinase activity J Clin Pharmacol (2007) 47, 1398-1407. PubMed Europe PubMed DOI I
Guertin,K.R. and Choi,Y.M. The discovery of the factor Xa inhibitor otamixaban: from lead identification to clinical development Curr Med Chem (2007) 14, 2471-2481. PubMed Europe PubMed DOI I
Kohrt,J.T., Bigge,C.F., Bryant,J.W., Casimiro-Garcia,A., Chi,L., Cody,W.L., Dahring,T., Dudley,D.A., Filipski,K.J., Haarer,S., Heemstra,R., Janiczek,N., Narasimhan,L., McClanahan,T., Peterson,J.T., Sahasrabudhe,V., Schaum,R., Van Huis,C.A., Welch,K.M., Zhang,E., Leadley,R.J. and Edmunds,J.J. The discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an orally efficacious factor Xa inhibitor Chem Biol Drug Des (2007) 70, 100-112. PubMed Europe PubMed DOI I
Levigne,S., Thiec,F., Cherel,G., Irving,J.A., Fribourg,C. and Christophe,O.D. Role of the alpha-helix 163-170 in factor Xa catalytic activity J Biol Chem (2007) 282, 31569-31579. PubMed Europe PubMed DOI
Murakami,M.T., Rios-Steiner,J., Weaver,S.E., Tulinsky,A., Geiger,J.H. and Arni,R.K. Intermolecular interactions and characterization of the novel factor Xa exosite involved in macromolecular recognition and inhibition: crystal structure of human Gla-domainless factor Xa complexed with the anticoagulant protein NAPc2 from the hematophagous nematode Ancylostoma caninum J Mol Biol (2007) 366, 602-610. PubMed Europe PubMed DOI S
Nagata,T., Yoshino,T., Haginoya,N., Yoshikawa,K., Isobe,Y., Furugohri,T. and Kanno,H. Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors Bioorg Med Chem Lett (2007) 17, 4683-4688. PubMed Europe PubMed DOI I
Pinto,D.J., Orwat,M.J., Koch,S., Rossi,K.A., Alexander,R.S., Smallwood,A., Wong,P.C., Rendina,A.R., Luettgen,J.M., Knabb,R.M., He,K., Xin,B., Wexler,R.R. and Lam,P.Y. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa J Med Chem (2007) 50, 5339-5356. PubMed Europe PubMed DOI I
Qiao,J.X., Chang,C.H., Cheney,D.L., Morin,P.E., Wang,G.Z., King,S.R., Wang,T.C., Rendina,A.R., Luettgen,J.M., Knabb,R.M., Wexler,R.R. and Lam,P.Y. SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation factor Xa Bioorg Med Chem Lett (2007) 17, 4419-4427. PubMed Europe PubMed DOI S I
Rios-Steiner,J.L., Murakami,M.T., Tulinsky,A. and Arni,R.K. Active and exo-site inhibition of human factor Xa: structure of des-Gla factor Xa inhibited by NAP5, a potent nematode anticoagulant protein from Ancylostoma caninum J Mol Biol (2007) 371, 774-786. PubMed Europe PubMed DOI S
Shinagawa,K., Martin,J.A., Ploplis,V.A. and Castellino,F.J. Coagulation factor Xa modulates airway remodeling in a murine model of asthma Am J Respir Crit Care Med (2007) 175, 136-143. PubMed Europe PubMed DOI PMC EPMC
Van Huis,C.A., Bigge,C.F., Casimiro-Garcia,A., Cody,W.L., Dudley,D.A., Filipski,K.J., Heemstra,R.J., Kohrt,J.T., Narasimhan,L.S., Schaum,R.P., Zhang,E., Bryant,J.W., Haarer,S., Janiczek,N., Leadley,R.J., Jr., McClanahan,T., Thomas Peterson,J., Welch,K.M. and Edmunds,J.J. Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors Chem Biol Drug Des (2007) 69, 444-450. PubMed Europe PubMed DOI S I
Weitz,J.I. Factor Xa or thrombin: is thrombin a better target? J Thromb Haemost (2007) 5 Suppl 1, 65-67. PubMed Europe PubMed DOI V T
Ye,B., Arnaiz,D.O., Chou,Y.L., Griedel,B.D., Karanjawala,R., Lee,W., Morrissey,M.M., Sacchi,K.L., Sakata,S.T., Shaw,K.J., Wu,S.C., Zhao,Z., Adler,M., Cheeseman,S., Dole,W.P., Ewing,J., Fitch,R., Lentz,D., Liang,A., Light,D., Morser,J., Post,J., Rumennik,G., Subramanyam,B., Sullivan,M.E., Vergona,R., Walters,J., Wang,Y.X., White,K.A., Whitlow,M. and Kochanny,M.J. Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors J Med Chem (2007) 50, 2967-2980. PubMed Europe PubMed DOI I
Young,R.J., Brown,D., Burns-Kurtis,C.L., Chan,C., Convery,M.A., Hubbard,J.A., Kelly,H.A., Pateman,A.J., Patikis,A., Senger,S., Shah,G.P., Toomey,J.R., Watson,N.S. and Zhou,P. Selective and dual action orally active inhibitors of thrombin and factor Xa Bioorg Med Chem Lett (2007) 17, 2927-2930. PubMed Europe PubMed DOI I

2006

[YEAR:28-3-2006]Auerswald,G. Prophylaxis in rare coagulation disorders-factor X deficiency Thromb Res (28-3-2006) 118 Suppl 1, S29-S31. PubMed Europe PubMed DOI
Becker,R.C., Alexander,J.H., Dyke,C., Huang,Y., Saint-Jacques,H., Hasselblad,V., Harrington,R.A. and Bovill,E.G. Effect of the novel direct factor Xa inhibitor DX-9065a on thrombin generation and inhibition among patients with stable atherosclerotic coronary artery disease Thromb Res (2006) 117, 439-446. PubMed Europe PubMed DOI I
[YEAR:6-5-2006]Fevig,J.M., Cacciola,J., Buriak,J., Jr., Rossi,K.A., Knabb,R.M., Luettgen,J.M., Wong,P.C., Bai,S.A., Wexler,R.R. and Lam,P.Y. Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa Bioorg Med Chem Lett (6-5-2006) 16, 3755-3760. PubMed Europe PubMed DOI I
Graefe-Mody,E.U., Schuhly,U., Rathgen,K., Stahle,H., Leitner,J.M. and Jilma,B. Pharmacokinetics and pharmacodynamics of BIBT 986, a novel small molecule dual inhibitor of thrombin and factor Xa J Thromb Haemost (2006) 4, 1502-1509. PubMed Europe PubMed DOI I
[YEAR:3-5-2006]Johnson,D.J., Li,W., Adams,T.E. and Huntington,J.A. Antithrombin-S195A factor Xa-heparin structure reveals the allosteric mechanism of antithrombin activation EMBO J (3-5-2006) 25, 2029-2037. PubMed Europe PubMed DOI PMC EPMC S
Kohrt,J.T., Filipski,K.J., Cody,W.L., Bigge,C.F., La,F., Welch,K., Dahring,T., Bryant,J.W., Leonard,D., Bolton,G., Narasimhan,L., Zhang,E., Peterson,J.T., Haarer,S., Sahasrabudhe,V., Janiczek,N., Desiraju,S., Hena,M., Fiakpui,C., Saraswat,N., Sharma,R., Sun,S., Maiti,S.N., Leadley,R. and Edmunds,J.J. The discovery of glycine and related amino acid-based factor Xa inhibitors Bioorg Med Chem (2006) 14, 4379-4392. PubMed Europe PubMed DOI S I
[YEAR:24-7-2006]Li,Y.L., Fevig,J.M., Cacciola,J., Buriak,J., Jr., Rossi,K.A., Jona,J., Knabb,R.M., Luettgen,J.M., Wong,P.C., Bai,S.A., Wexler,R.R. and Lam,P.Y. Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa Bioorg Med Chem Lett (24-7-2006) 16, 5176-5182. PubMed Europe PubMed DOI I
Matsushita,K., Imamura,T., Tancharoen,S., Tatsuyama,S., Tomikawa,M., Travis,J., Potempa,J., Torii,M. and Maruyama,I. Selective inhibition of Porphyromonas gingivalis growth by a factor Xa inhibitor, DX-9065a J Periodontal Res (2006) 41, 171-176. PubMed Europe PubMed DOI I
[YEAR:25-5-2006]Pinto,D.J., Orwat,M.J., Quan,M.L., Han,Q., Galemmo,R.A., Jr., Amparo,E., Wells,B., Ellis,C., He,M.Y., Alexander,R.S., Rossi,K.A., Smallwood,A., Wong,P.C., Luettgen,J.M., Rendina,A.R., Knabb,R.M., Mersinger,L., Kettner,C., Bai,S., He,K., Wexler,R.R. and Lam,P.Y. 1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa Bioorg Med Chem Lett (25-5-2006) 16, 4141-4147. PubMed Europe PubMed DOI I
[YEAR:8-9-2006]Pinto,D.J., Galemmo,R.A., Jr., Quan,M.L., Orwat,M.J., Clark,C., Li,R., Wells,B., Woerner,F., Alexander,R.S., Rossi,K.A., Smallwood,A., Wong,P.C., Luettgen,J.M., Rendina,A.R., Knabb,R.M., He,K., Wexler,R.R. and Lam,P.Y. Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties Bioorg Med Chem Lett (8-9-2006) 16, 5584-5589. PubMed Europe PubMed DOI I
Rezaie,A.R. Determinants of specificity of factor Xa interaction with its physiological inhibitors Mini Rev Med Chem (2006) 6, 859-865. PubMed Europe PubMed DOI
[YEAR:25-4-2006]Rezaie,A.R. Pentasaccharide enhances the inactivation of factor Xa by antithrombin by promoting the assembly of a Michaelis-type intermediate complex. Demonstration by rapid kinetic, surface plasmon resonance, and competitive binding studies Biochemistry (25-4-2006) 45, 5324-5329. PubMed Europe PubMed DOI PMC EPMC
Schweinitz,A., Sturzebecher,A., Sturzebecher,U., Schuster,O., Sturzebecher,J. and Steinmetzer,T. New substrate analogue inhibitors of factor Xa containing 4-amidinobenzylamide as P1 residue: part 1 Med Chem (2006) 2, 349-361. PubMed Europe PubMed DOI I
Senger,S., Convery,M.A., Chan,C. and Watson,N.S. Arylsulfonamides: a study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors Bioorg Med Chem Lett (2006) 16, 5731-5735. PubMed Europe PubMed DOI I
Siigur,J. and Siigur,E. Factor X activating proteases from snake venoms J Toxicol Toxin Rev (2006) 25, 235-255. V
Watson,N.S., Brown,D., Campbell,M., Chan,C., Chaudry,L., Convery,M.A., Fenwick,R., Hamblin,J.N., Haslam,C., Kelly,H.A., King,N.P., Kurtis,C.L., Leach,A.R., Manchee,G.R., Mason,A.M., Mitchell,C., Patel,C., Patel,V.K., Senger,S., Shah,G.P., Weston,H.E., Whitworth,C. and Young,R.J. Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors Bioorg Med Chem Lett (2006) 16, 3784-3788. PubMed Europe PubMed DOI S I
Young,R.J., Campbell,M., Borthwick,A.D., Brown,D., Burns-Kurtis,C.L., Chan,C., Convery,M.A., Crowe,M.C., Dayal,S., Diallo,H., Kelly,H.A., King,N.P., Kleanthous,S., Mason,A.M., Mordaunt,J.E., Patel,C., Pateman,A.J., Senger,S., Shah,G.P., Smith,P.W., Watson,N.S., Weston,H.E. and Zhou,P. Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs Bioorg Med Chem Lett (2006) 16, 5953-5957. PubMed Europe PubMed DOI I

2005

Banke,I.J., Arlt,M.J., Mueller,M.M., Sperl,S., Stemberger,A., Sturzebecher,J., Amirkhosravi,A., Moroder,L. and Kruger,A. Effective inhibition of experimental metastasis and prolongation of survival in mice by a potent factor Xa-specific synthetic serine protease inhibitor with weak anticoagulant activity Thromb Haemost (2005) 94, 1084-1093. PubMed Europe PubMed DOI I
[YEAR:19-7-2005]Bianchini,E.P., Orcutt,S.J., Panizzi,P., Bock,P.E. and Krishnaswamy,S. Ratcheting of the substrate from the zymogen to proteinase conformations directs the sequential cleavage of prothrombin by prothrombinase Proc Natl Acad Sci U S A (19-7-2005) 102, 10099-10104. PubMed Europe PubMed DOI PMC EPMC
[YEAR:1-9-2005]Franciskovich,J.B., Masters,J.J., Tinsley,J.M., Craft,T.J., Froelich,L.L., Gifford-Moore,D.S., Klimkowski,V.J., Smallwood,J.K., Smith,G.F., Smith,T., Towner,R.R., Weir,L.C. and Wiley,M.R. Investigation of factor Xa inhibitors containing non-amidine S1 elements Bioorg Med Chem Lett (1-9-2005) 15, 4838-4841. PubMed Europe PubMed DOI I
Komoriya,S., Haginoya,N., Kobayashi,S., Nagata,T., Mochizuki,A., Suzuki,M., Yoshino,T., Horino,H., Nagahara,T., Suzuki,M., Isobe,Y. and Furugoori,T. Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites Bioorg Med Chem (2005) 13, 3927-3954. PubMed Europe PubMed DOI S I
[YEAR:15-2-2005]Koshio,H., Hirayama,F., Ishihara,T., Shiraki,R., Shigenaga,T., Taniuchi,Y., Sato,K., Moritani,Y., Iwatsuki,Y., Kaku,S., Katayama,N., Kawasaki,T., Matsumoto,Y., Sakamoto,S. and Tsukamoto,S. Synthesis and biological activity of novel 1,2-disubstituted benzene derivatives as factor Xa inhibitors Bioorg Med Chem (15-2-2005) 13, 1305-1323. PubMed Europe PubMed DOI I
Kumar,A., Mishra,K.L., Kumar,A. and Mishra,D. Hereditary coagulation factor X deficiency Indian Pediatr (2005) 42, 1240-1242. PubMed Europe PubMed M
[YEAR:2-8-2005]Manithody,C. and Rezaie,A.R. Functional mapping of charged residues of the 82-116 sequence in factor Xa: evidence that lysine 96 is a factor Va independent recognition site for prothrombin in the prothrombinase complex Biochemistry (2-8-2005) 44, 10063-10070. PubMed Europe PubMed DOI
[YEAR:5-5-2005]Matter,H., Will,D.W., Nazare,M., Schreuder,H., Laux,V. and Wehner,V. Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions J Med Chem (5-5-2005) 48, 3290-3312. PubMed Europe PubMed DOI I
Nazare,M., Will,D.W., Matter,H., Schreuder,H., Ritter,K., Urmann,M., Essrich,M., Bauer,A., Wagner,M., Czech,J., Lorenz,M., Laux,V. and Wehner,V. Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography J Med Chem (2005) 48, 4511-4525. PubMed Europe PubMed DOI S I
Quan,M.L., Lam,P.Y., Han,Q., Pinto,D.J., He,M.Y., Li,R., Ellis,C.D., Clark,C.G., Teleha,C.A., Sun,J.H., Alexander,R.S., Bai,S., Luettgen,J.M., Knabb,R.M., Wong,P.C. and Wexler,R.R. Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor J Med Chem (2005) 48, 1729-1744. PubMed Europe PubMed DOI I
Reza,A., Swarup,S. and Manjunatha Kini,R. Two parallel prothrombin activator systems in Australian rough-scaled snake, Tropidechis carinatus. Structural comparison of venom prothrombin activator with blood coagulation factor X Thromb Haemost (2005) 93, 40-47. PubMed Europe PubMed DOI
Reza,M.A., Swarup,S. and Kini,R.M. Gene structures of trocarin D and coagulation factor X, two functionally diverse prothrombin activators from Australian rough scaled snake Pathophysiol Haemost Thromb (2005) 34, 205-208. PubMed Europe PubMed DOI
[YEAR:3-8-2005]Rezaie,A.R., Manithody,C. and Yang,L. Identification of factor Xa residues critical for interaction with protein Z-dependent protease inhibitor: both active site and exosite interactions are required for inhibition J Biol Chem (3-8-2005) 280, 32722-32728. PubMed Europe PubMed DOI PMC EPMC
Scharer,K., Morgenthaler,M., Paulini,R., Obst-Sander,U., Banner,D.W., Schlatter,D., Benz,J., Stihle,M. and Diederich,F. Quantification of cation-pi interactions in protein-ligand complexes: crystal-structure analysis of factor Xa bound to a quaternary ammonium ion ligand Angew Chem Int Ed Engl (2005) 44, 4400-4404. PubMed Europe PubMed DOI S
Volkel,T., Heidtmann,H.H., Muller,R. and Kontermann,R.E. Engineering of human coagulation factor X variants activated by prostate-specific antigen Mol Biotechnol (2005) 29, 19-30. PubMed Europe PubMed DOI

2004

[YEAR:1-11-2004]Batt,D.G., Qiao,J.X., Modi,D.P., Houghton,G.C., Pierson,D.A., Rossi,K.A., Luettgen,J.M., Knabb,R.M., Jadhav,P.K. and Wexler,R.R. 5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa Bioorg Med Chem Lett (1-11-2004) 14, 5269-5273. PubMed Europe PubMed DOI I
Becker,R.C., Alexander,J., Dyke,C.K. and Harrington,R.A. Development of DX-9065a, a novel direct factor Xa antagonist, in cardiovascular disease Thromb Haemost (2004) 92, 1182-1193. PubMed Europe PubMed DOI I
Brown,M.A., Stenberg,L.M. and Stenflo,J. Coagulation factor X [ISSN:0-12-079610-4] (2004) 2, 1662-1666. V
Girolami,A., Vianello,F., Cabrio,L. and Lombardi,A.M. A new mutation (Arg251Trp) in the Ca2+ binding site of factor X protease domain appears to be responsible for the defect in the extrinsic pathway activation of factor X Padua Clin Appl Thromb Hemost (2004) 10, 5-8. PubMed Europe PubMed
Haginoya,N., Kobayashi,S., Komoriya,S., Yoshino,T., Suzuki,M., Shimada,T., Watanabe,K., Hirokawa,Y., Furugori,T. and Nagahara,T. Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element J Med Chem (2004) 47, 5167-5182. PubMed Europe PubMed DOI S I
Ieko,M., Tarumi,T., Takeda,M., Naito,S., Nakabayashi,T. and Koike,T. Synthetic selective inhibitors of coagulation factor Xa strongly inhibit thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis J Thromb Haemost (2004) 2, 612-618. PubMed Europe PubMed DOI I
[YEAR:1-5-2004]Komoriya,S., Kanaya,N., Nagahara,T., Yokoyama,A., Inamura,K., Yokoyama,Y., Katakura,S. and Hara,T. Design, synthesis and biological activity of amidinobicyclic compounds (derivatives of DX-9065a) as factor Xa inhibitors: SAR study of S1 and aryl binding sites Bioorg Med Chem (1-5-2004) 12, 2099-2114. PubMed Europe PubMed DOI V I
[YEAR:1-5-2004]Koshio,H., Hirayama,F., Ishihara,T., Taniuchi,Y., Sato,K., Sakai-Moritani,Y., Kaku,S., Kawasaki,T., Matsumoto,Y., Sakamoto,S. and Tsukamoto,S. Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity Bioorg Med Chem (1-5-2004) 12, 2179-2191. PubMed Europe PubMed DOI I
[YEAR:15-10-2004]Koshio,H., Hirayama,F., Ishihara,T., Kaizawa,H., Shigenaga,T., Taniuchi,Y., Sato,K., Moritani,Y., Iwatsuki,Y., Uemura,T., Kaku,S., Kawasaki,T., Matsumoto,Y., Sakamoto,S. and Tsukamoto,S. Orally active factor Xa inhibitor: synthesis and biological activity of masked amidines as prodrugs of novel 1,4-diazepane derivatives Bioorg Med Chem (15-10-2004) 12, 5415-5426. PubMed Europe PubMed DOI I
Kranjc,A. and Kikelj,D. Dual inhibitors of the blood coagulation enzymes Curr Med Chem (2004) 11, 2535-2547. PubMed Europe PubMed
[YEAR:6-12-2004]Mederski,W.W., Cezanne,B., van Amsterdam,C., Buhring,K.U., Dorsch,D., Gleitz,J., Marz,J. and Tsaklakidis,C. Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa Bioorg Med Chem Lett (6-12-2004) 14, 5817-5822. PubMed Europe PubMed DOI I
[YEAR:7-6-2004]Nazare,M., Matter,H., Klingler,O., Al-Obeidi,F., Schreuder,H., Zoller,G., Czech,J., Lorenz,M., Dudda,A., Peyman,A., Nestler,H.P., Urmann,M., Bauer,A., Laux,V., Wehner,V. and Will,D.W. Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand Bioorg Med Chem Lett (7-6-2004) 14, 2801-2805. PubMed Europe PubMed DOI I
[YEAR:24-12-2004]Orcutt,S.J. and Krishnaswamy,S. Binding of substrate in two conformations to human prothrombinase drives consecutive cleavage at two sites in prothrombin J Biol Chem (24-12-2004) 279, 54927-54936. PubMed Europe PubMed DOI
[YEAR:16-3-2004]Rezaie,A.R., Yang,L. and Manithody,C. Mutagenesis studies toward understanding the mechanism of differential reactivity of factor Xa with the native and heparin-activated antithrombin Biochemistry (16-3-2004) 43, 2898-2905. PubMed Europe PubMed DOI
[YEAR:30-3-2004]Rezaie,A.R. Kinetics of factor Xa inhibition by recombinant tick anticoagulant peptide: both active site and exosite interactions are required for a slow- and tight-binding inhibition mechanism Biochemistry (30-3-2004) 43, 3368-3375. PubMed Europe PubMed DOI
[YEAR:18-10-2004]Rumthao,S., Lee,O., Sheng,Q., Fu,W., Mulhearn,D.C., Crich,D., Mesecar,A.D. and Johnson,M.E. Design, synthesis, and evaluation of oxyanion-hole selective inhibitor substituents for the S1 subsite of factor Xa Bioorg Med Chem Lett (18-10-2004) 14, 5165-5170. PubMed Europe PubMed DOI I
[YEAR:29-7-2004]Willardsen,J.A., Dudley,D.A., Cody,W.L., Chi,L., McClanahan,T.B., Mertz,T.E., Potoczak,R.E., Narasimhan,L.S., Holland,D.R., Rapundalo,S.T. and Edmunds,J.J. Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa J Med Chem (29-7-2004) 47, 4089-4099. PubMed Europe PubMed DOI I

2003

[YEAR:28-2-2003]Brufatto,N. and Nesheim,M.E. Analysis of the kinetics of prothrombin activation and evidence that two equilibrating forms of prothrombinase are involved in the process J Biol Chem (28-2-2003) 278, 6755-6764. PubMed Europe PubMed DOI
[YEAR:27-2-2003]Choi-Sledeski,Y.M., Kearney,R., Poli,G., Pauls,H., Gardner,C., Gong,Y., Becker,M., Davis,R., Spada,A., Liang,G., Chu,V., Brown,K., Collussi,D., Leadley,R., Jr., Rebello,S., Moxey,P., Morgan,S., Bentley,R., Kasiewski,C., Maignan,S., Guilloteau,J.P. and Mikol,V. Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand J Med Chem (27-2-2003) 46, 681-684. PubMed Europe PubMed DOI I
Jenny,R.J., Mann,K.G. and Lundblad,R.L. A critical review of the methods for cleavage of fusion proteins with thrombin and factor Xa Protein Expr Purif (2003) 31, 1-11. PubMed Europe PubMed DOI
[YEAR:25-6-2003]Josic,D., Hoffer,L. and Buchacher,A. Preparation of vitamin K-dependent proteins, such as clotting factors II, VII, IX and X and clotting inhibitor protein C J Chromatogr B Analyt Technol Biomed Life Sci (25-6-2003) 790, 183-197. PubMed Europe PubMed DOI
Ludeman,J.P., Pike,R.N., Bromfield,K.M., Duggan,P.J., Cianci,J., Le Bonniec,B., Whisstock,J.C. and Bottomley,S.P. Determination of the P1', P2' and P3' subsite-specificity of factor Xa Int J Biochem Cell Biol (2003) 35, 221-225. PubMed Europe PubMed DOI
Maignan,S., Guilloteau,J.P., Choi-Sledeski,Y.M., Becker,M.R., Ewing,W.R., Pauls,H.W., Spada,A.P. and Mikol,V. Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket J Med Chem (2003) 46, 685-690. PubMed Europe PubMed DOI S I
Nogami,K., Wakabayashi,H. and Fay,P.J. Mechanisms of factor Xa-catalyzed cleavage of the factor VIIIa A1 subunit resulting in cofactor inactivation J Biol Chem (2003) 278, 16502-16509. PubMed Europe PubMed DOI
Oliva,M.L., Andrade,S.A., Juliano,M.A., Sallai,R.C., Torquato,R.J., Sampaio,M.U., Pott,V.J. and Sampaio,C.A. Kinetic characterization of factor Xa binding using a quenched fluorescent substrate based on the reactive site of factor Xa inhibitor from Bauhinia ungulata seeds Curr Med Chem (2003) 10, 1085-1093. PubMed Europe PubMed DOI
[YEAR:31-1-2003]Reyda,S., Sohn,C., Klebe,G., Rall,K., Ullmann,D., Jakubke,H.D. and Stubbs,M.T. Reconstructing the binding site of factor Xa in trypsin reveals ligand-induced structural plasticity J Mol Biol (31-1-2003) 325, 963-977. PubMed Europe PubMed DOI
[YEAR:21-7-2003]Ries,U.J., Priepke,H.W., Hauel,N.H., Handschuh,S., Mihm,G., Stassen,J.M., Wienen,W. and Nar,H. Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents Bioorg Med Chem Lett (21-7-2003) 13, 2297-2302. PubMed Europe PubMed DOI I
Sinha,U., Lin,P.H., Edwards,S.T., Wong,P.W., Zhu,B., Scarborough,R.M., Su,T., Jia,Z.J., Song,Y., Zhang,P., Clizbe,L., Park,G., Reed,A., Hollenbach,S.J., Malinowski,J. and Arfsten,A.E. Inhibition of purified factor Xa amidolytic activity may not be predictive of inhibition of in vivo thrombosis: implications for identification of therapeutically active inhibitors Arterioscler Thromb Vasc Biol (2003) 23, 1098-1104. PubMed Europe PubMed DOI I
[YEAR:21-3-2003]Thiec,F., Cherel,G. and Christophe,O.D. Role of the Gla and first epidermal growth factor-like domains of factor X in the prothrombinase and tissue factor-factor VIIa complexes J Biol Chem (21-3-2003) 278, 10393-10399. PubMed Europe PubMed DOI
Tomokiyo,K., Nakatomi,Y., Araki,T., Teshima,K., Nakano,H., Nakagaki,T., Miyamoto,S., Funatsu,A. and Iwanaga,S. A novel therapeutic approach combining human plasma-derived factors VIIa and X for haemophiliacs with inhibitors: evidence of a higher thrombin generation rate in vitro and more sustained haemostatic activity in vivo than obtained with factor VIIa alone Vox Sang (2003) 85, 290-299. PubMed Europe PubMed DOI
[YEAR:8-7-2003]Wang,S.X., Hur,E., Sousa,C.A., Brinen,L., Slivka,E.J. and Fletterick,R.J. The extended interactions and Gla domain of blood coagulation factor Xa Biochemistry (8-7-2003) 42, 7959-7966. PubMed Europe PubMed DOI S

2002

Adler,M., Kochanny,M.J., Ye,B., Rumennik,G., Light,D.R., Biancalana,S. and Whitlow,M. Crystal structures of two potent nonamidine inhibitors bound to factor Xa Biochemistry (2002) 41, 15514-15523. PubMed Europe PubMed DOI S I
[YEAR:22-1-2002]Banerjee,M., Majumder,R., Weinreb,G., Wang,J. and Lentz,B.R. Role of procoagulant lipids in human prothrombin activation. 2. Soluble phosphatidylserine upregulates and directs factor X(a) to appropriate peptide bonds in prothrombin Biochemistry (22-1-2002) 41, 950-957. PubMed Europe PubMed DOI
Bianchini,E.P., Louvain,V.B., Marque,P.E., Juliano,M.A., Juliano,L. and le Bonniec,B.F. Mapping of the catalytic groove preferences of factor Xa reveals an inadequate selectivity for its macromolecule substrates J Biol Chem (2002) 277, 20527-20534. PubMed Europe PubMed DOI P
[YEAR:4-10-2002]Camire,R.M. Prothrombinase assembly and S1 site occupation restore the catalytic activity of FXa impaired by mutation at the sodium-binding site J Biol Chem (4-10-2002) 277, 37863-37870. PubMed Europe PubMed DOI
[YEAR:1-4-2002]Edwards,S.T., Betz,A., James,H.L., Thompson,E., Yonkovich,S.J. and Sinha,U. Differences between human and rabbit coagulation factor X - implications for in vivo models of thrombosis Thromb Res (1-4-2002) 106, 71-79. PubMed Europe PubMed DOI
Guertin,K.R., Gardner,C.J., Klein,S.I., Zulli,A.L., Czekaj,M., Gong,Y., Spada,A.P., Cheney,D.L., Maignan,S., Guilloteau,J.P., Brown,K.D., Colussi,D.J., Chu,V., Heran,C.L., Morgan,S.R., Bentley,R.G., Dunwiddie,C.T., Leadley,R.J. and Pauls,H.W. Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity Bioorg Med Chem Lett (2002) 12, 1671-1674. PubMed Europe PubMed DOI I
[YEAR:22-2-2002]Harrison,L.M., Nerlinger,A., Bungiro,R.D., Cordova,J.L., Kuzmic,P. and Cappello,M. Molecular characterization of Ancylostoma inhibitors of coagulation factor Xa. Hookworm anticoagulant activity in vitro predicts parasite bloodfeeding in vivo J Biol Chem (22-2-2002) 277, 6223-6229. PubMed Europe PubMed DOI
Liebeschuetz,J.W., Jones,S.D., Morgan,P.J., Murray,C.W., Rimmer,A.D., Roscoe,J.M., Waszkowycz,B., Welsh,P.M., Wylie,W.A., Young,S.C., Martin,H., Mahler,J., Brady,L. and Wilkinson,K. PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors J Med Chem (2002) 45, 1221-1232. PubMed Europe PubMed DOI I
Matsuda,Y., Shimokawa,K., Katayama,M., Shimizu,H., Umeda,T., Oshio,S. and Chiba,R. Blood coagulation factor X (FX) in human seminal plasma Arch Androl (2002) 48, 295-300. PubMed Europe PubMed DOI
[YEAR:20-6-2002]Matter,H., Defossa,E., Heinelt,U., Blohm,P.M., Schneider,D., Muller,A., Herok,S., Schreuder,H., Liesum,A., Brachvogel,V., Lonze,P., Walser,A., Al-Obeidi,F. and Wildgoose,P. Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa J Med Chem (20-6-2002) 45, 2749-2769. PubMed Europe PubMed DOI I
Mueller,M.M., Sperl,S., Sturzebecher,J., Bode,W. and Moroder,L. (R)-3-Amidinophenylalanine-derived inhibitors of factor Xa with a novel active-site binding mode Biol Chem (2002) 383, 1185-1191. PubMed Europe PubMed DOI S I
Petitou,M., Duchaussoy,P., Herbert,J.M., Duc,G., El Hajji,M., Branellec,J.F., Donat,F., Necciari,J., Cariou,R., Bouthier,J. and Garrigou,E. The synthetic pentasaccharide fondaparinux: first in the class of antithrombotic agents that selectively inhibit coagulation factor Xa Semin Thromb Hemost (2002) 28, 393-402. PubMed Europe PubMed DOI I
[YEAR:6-5-2002]Shaw,K.J., Guilford,W.J., Griedel,B.D., Sakata,S., Trinh,L., Wu,S., Xu,W., Zhao,Z. and Morrissey,M.M. Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity Bioorg Med Chem Lett (6-5-2002) 12, 1311-1314. PubMed Europe PubMed DOI I
Steen,M. Factor Va-factor Xa interactions: molecular sites involved in enzyme:cofactor assembly Scand J Clin Lab Invest Suppl (2002) 237, 5-11. PubMed Europe PubMed
Venkateswarlu,D., Perera,L., Darden,T. and Pedersen,L.G. Structure and dynamics of zymogen human blood coagulation factor X Biophys J (2002) 82, 1190-1206. PubMed Europe PubMed DOI PMC EPMC
[YEAR:22-1-2002]Wu,J.R., Zhou,C., Majumder,R., Powers,D.D., Weinreb,G. and Lentz,B.R. Role of procoagulant lipids in human prothrombin activation. 1. Prothrombin activation by factor X(a) in the absence of factor Va and in the absence and presence of membranes Biochemistry (22-1-2002) 41, 935-949. PubMed Europe PubMed DOI
[YEAR:1-2-2002]Zhong,D., Bajaj,M.S., Schmidt,A.E. and Bajaj,S.P. The N-terminal epidermal growth factor-like domain in factor IX and factor X represents an important recognition motif for binding to tissue factor J Biol Chem (1-2-2002) 277, 3622-3631. PubMed Europe PubMed DOI

2001

Monno,R., Grandaliano,G., Faccio,R., Ranieri,E., Martino,C., Gesualdo,L. and Schena,F.P. Activated coagulation factor X: A novel mitogenic stimulus for human mesangial cells J Am Soc Nephrol (2001) 12, 891-899. PubMed Europe PubMed
[YEAR:15-2-2001]Pinto,D.J., Orwat,M.J., Wang,S., Fevig,J.M., Quan,M.L., Amparo,E., Cacciola,J., Rossi,K.A., Alexander,R.S., Smallwood,A.M., Luettgen,J.M., Liang,L., Aungst,B.J., Wright,M.R., Knabb,R.M., Wong,P.C., Wexler,R.R. and Lam,P.Y. Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4 -yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa J Med Chem (15-2-2001) 44, 566-578. PubMed Europe PubMed DOI I
Rai,R., Sprengeler,P.A., Elrod,K.C. and Young,W.B. Perspectives on factor Xa inhibition Curr Med Chem (2001) 8, 101-119. PubMed Europe PubMed
[YEAR:15-4-2001]Rezaie,A.R. Prothrombin protects factor Xa in the prothrombinase complex from inhibition by the heparin-antithrombin complex Blood (15-4-2001) 97, 2308-2313. PubMed Europe PubMed DOI
[YEAR:3-10-2001]Rezaie,A.R. and Yang,L. Probing the molecular basis of factor Xa specificity by mutagenesis of the serpin, antithrombin Biochim Biophys Acta (3-10-2001) 1528, 167-176. PubMed Europe PubMed DOI
[YEAR:23-7-2001]Shrader,W.D., Young,W.B., Sprengeler,P.A., Sangalang,J.C., Elrod,K. and Carr,G. Neutral inhibitors of the serine protease factor Xa Bioorg Med Chem Lett (23-7-2001) 11, 1801-1804. PubMed Europe PubMed DOI I

2000

[YEAR:17-10-2000]Adler,M., Davey,D.D., Phillips,G.B., Kim,S.H., Jancarik,J., Rumennik,G., Light,D.R. and Whitlow,M. Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa Biochemistry (17-10-2000) 39, 12534-12542. PubMed Europe PubMed DOI S I
[YEAR:21-11-2000]Camire,R.M., Larson,P.J., Stafford,D.W. and High,K.A. Enhanced gamma-carboxylation of recombinant factor X using a chimeric construct containing the prothrombin propeptide Biochemistry (21-11-2000) 39, 14322-14329. PubMed Europe PubMed DOI
Dewerchin,M., Liang,Z., Moons,L., Carmeliet,P., Castellino,F.J., Collen,D. and Rosen,E.D. Blood coagulation factor X deficiency causes partial embryonic lethality and fatal neonatal bleeding in mice Thromb Haemost (2000) 83, 185-190. PubMed Europe PubMed K
[YEAR:5-7-2000]Harris,J.L., Backes,B.J., Leonetti,F., Mahrus,S., Ellman,J.A. and Craik,C.S. Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries Proc Natl Acad Sci U S A (5-7-2000) 97, 7754-7759. PubMed Europe PubMed DOI PMC EPMC P
Katz,B.A., Mackman,R., Luong,C., Radika,K., Martelli,A., Sprengeler,P.A., Wang,J., Chan,H. and Wong,L. Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator Chem Biol (2000) 7, 299-312. PubMed Europe PubMed DOI S
Maignan,S., Guilloteau,J.P., Pouzieux,S., Choi-Sledeski,Y.M., Becker,M.R., Klein,S.I., Ewing,W.R., Pauls,H.W., Spada,A.P. and Mikol,V. Crystal structures of human factor Xa complexed with potent inhibitors J Med Chem (2000) 43, 3226-3232. PubMed Europe PubMed DOI S I
Poorafshar,M., Aveskogh,M., Munday,B. and Hellman,L. Identification and structural analysis of four serine proteases in a monotreme, the platypus, Ornithorhynchus anatinus Immunogenetics (2000) 52, 19-28. PubMed Europe PubMed DOI
[YEAR:22-2-2000]Rezaie,A.R. and He,X. Sodium binding site of factor Xa: Role of sodium in the prothrombinase complex Biochemistry (22-2-2000) 39, 1817-1825. PubMed Europe PubMed DOI
Sperl,S., Bergner,A., Sturzebecher,J., Magdolen,V., Bode,W. and Moroder,L. Urethanyl-3-amidinophenylalanine derivatives as inhibitors of factor Xa. X-ray crystal structure of a trypsin/inhibitor complex and modeling studies Biol Chem (2000) 381, 321-329. PubMed Europe PubMed DOI S I
[YEAR:24-11-2000]Underwood,M.C., Zhong,D., Mathur,A., Heyduk,T. and Bajaj,S.P. Thermodynamic linkage between the S1 site, the Na+ site, and the Ca2+ site in the protease domain of human coagulation factor Xa. Studies on catalytic efficiency and inhibitor binding J Biol Chem (24-11-2000) 275, 36876-36884. PubMed Europe PubMed DOI I
Wilberding,J.A. and Castellino,F.J. Characterization of the murine coagulation factor X promoter Thromb Haemost (2000) 84, 1031-1038. PubMed Europe PubMed

1999

[YEAR:5-11-1999]Camerer,E., Rottingen,J.A., Gjernes,E., Larsen,K., Skartlien,A.H., Iversen,J.G. and Prydz,H. Coagulation factors VIIa and Xa induce cell signaling leading to up-regulation of the egr-1 gene J Biol Chem (5-11-1999) 274, 32225-32233. PubMed Europe PubMed DOI
[YEAR:9-9-1999]Ewing,W.R., Becker,M.R., Manetta,V.E., Davis,R.S., Pauls,H.W., Mason,H., Choi-Sledeski,Y.M., Green,D., Cha,D., Spada,A.P., Cheney,D.L., Mason,J.S., Maignan,S., Guilloteau,J.P., Brown,K., Colussi,D., Bentley,R., Bostwick,J., Kasiewski,C.J., Morgan,S.R., Leadley,R.J., Dunwiddie,C.T., Perrone,M.H. and Chu,V. Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa J Med Chem (9-9-1999) 42, 3557-3571. PubMed Europe PubMed DOI I
[YEAR:19-4-1999]Fevig,J.M., Buriak,J., Jr., Stouten,P.F., Knabb,R.M., Lam,G.N., Wong,P.C. and Wexler,R.R. Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa Bioorg Med Chem Lett (19-4-1999) 9, 1195-1200. PubMed Europe PubMed DOI I
Kaiser,B., Jeske,W., Walenga,J.M. and Fareed,J. Inactivation of factor Xa by the synthetic inhibitor DX-9065a causes strong anticoagulant and antiplatelet actions in human blood Blood Coagul Fibrinolysis (1999) 10, 495-501. PubMed Europe PubMed I
Leadley,R.J., Jr., Morgan,S.R., Bentley,R., Bostwick,J.S., Kasiewski,C.J., Heran,C., Chu,V., Brown,K., Moxey,P., Ewing,W.R., Pauls,H., Spada,A.P., Perrone,M.H. and Dunwiddie,C.T. Pharmacodynamic activity and antithrombotic efficacy of RPR120844, a novel inhibitor of coagulation factor Xa J Cardiovasc Pharmacol (1999) 34, 791-799. PubMed Europe PubMed DOI I
Sanderson,P.E. Small, noncovalent serine protease inhibitors Med Res Rev (1999) 19, 179-197. PubMed Europe PubMed DOI V I

1998

[YEAR:1-10-1998]Heidtmann,H.H. and Kontermann,R.E. Cloning and recombinant expression of mouse coagulation factor X Thromb Res (1-10-1998) 92, 33-41. PubMed Europe PubMed DOI
[YEAR:9-6-1998]Kamata,K., Kawamoto,H., Honma,T., Iwama,T. and Kim,S.H. Structural basis for chemical inhibition of human blood coagulation factor Xa Proc Natl Acad Sci U S A (9-6-1998) 95, 6630-6635. PubMed Europe PubMed DOI PMC EPMC
[YEAR:7-4-1998]Larson,P.J., Camire,R.M., Wong,D., Fasano,N.C., Monroe,D.M., Tracy,P.B. and High,K.A. Structure/function analyses of recombinant variants of human factor Xa: factor Xa incorporation into prothrombinase on the thrombin-activated platelet surface is not mimicked by synthetic phospholipid vesicles Biochemistry (7-4-1998) 37, 5029-5038. PubMed Europe PubMed DOI
Liang,Z., Cooper,A., DeFord,M.E., Carmeliet,P., Collen,D., Castellino,F.J. and Rosen,E.D. Cloning and characterization of a cDNA encoding murine coagulation factor X Thromb Haemost (1998) 80, 87-91. PubMed Europe PubMed
[YEAR:8-5-1998]Long,G.L., Lu,D., Xie,R.L. and Kalafatis,M. Human protein S cleavage and inactivation by coagulation factor Xa J Biol Chem (8-5-1998) 273, 11521-11526. PubMed Europe PubMed DOI
[YEAR:9-1-1998]Nakata,M., Kanekura,S. and Maruyama,I. DX9065a, an Xa inhibitor, inhibits prothrombin-induced A549 lung adenocarcinoma cell proliferation Cancer Lett (9-1-1998) 122, 127-133. PubMed Europe PubMed DOI I
Salemink,I., Franssen,J., Willems,G.M., Hemker,H.C., Li,A., Wun,T.C. and Lindhout,T. Factor Xa cleavage of tissue factor pathway inhibitor is associated with loss of anticoagulant activity Thromb Haemost (1998) 80, 273-280. PubMed Europe PubMed

1997

Bode,W., Brandstetter,H., Mather,T. and Stubbs,M.T. Comparative analysis of haemostatic proteinases: structural aspects of thrombin, factor Xa, factor IXa and protein C Thromb Haemost (1997) 78, 501-511. PubMed Europe PubMed
[YEAR:13-6-1997]Burgering,M.J., Orbons,L.P., van der Doelen,A., Mulders,J., Theunissen,H.J., Grootenhuis,P.D., Bode,W., Huber,R. and Stubbs,M.T. The second Kunitz domain of human tissue factor pathway inhibitor: cloning, structure determination and interaction with factor Xa J Mol Biol (13-6-1997) 269, 395-407. PubMed Europe PubMed DOI S
Butenas,S., DiLorenzo,M.E. and Mann,K.G. Ultrasensitive fluorogenic substrates for serine proteases Thromb Haemost (1997) 78, 1193-1201. PubMed Europe PubMed A
[YEAR:17-11-1997]Hopfner,K.P., Brandstetter,H., Karcher,A., Kopetzki,E., Huber,R., Engh,R.A. and Bode,W. Converting blood coagulation factor IXa into factor Xa: dramatic increase in amidolytic activity identifies important active site determinants EMBO J (17-11-1997) 16, 6626-6635. PubMed Europe PubMed DOI PMC EPMC
Imamura,T., Potempa,J., Tanase,S. and Travis,J. Activation of blood coagulation factor X by arginine-specific cysteine proteinases (gingipain-Rs) from Porphyromonas gingivalis J Biol Chem (1997) 272, 16062-16067. PubMed Europe PubMed DOI
James,H.L., Larson,P.J., Chao,Y.B., Yan,S.B. and Kim,D.J. Isolation and characterization of mouse coagulation factor X - Biophysical and enzymological properties Thromb Haemost (1997) 78, 1049-1054. PubMed Europe PubMed
Katoh,T., Tamaki,M., Kikuchi,N., Teraoka,H., Nagata,K. and Yoshida,N. Mutations within the reactive-site region of human pancreatic secretory trypsin inhibitor confer alpha-thrombin and factor Xa inhibitory activities Biosci Biotechnol Biochem (1997) 61, 389-391. PubMed Europe PubMed DOI
Krishnaswamy,S. and Betz,A. Exosites determine macromolecular substrate recognition by prothrombinase Biochemistry (1997) 36, 12080-12086. PubMed Europe PubMed DOI
Rudolph,A.E., Mullane,M.P., Porche-Sorbet,R. and Miletich,J.P. Expression, purification, and characterization of recombinant human factor X Protein Expr Purif (1997) 10, 373-378. PubMed Europe PubMed DOI E

1996

[YEAR:22-11-1996]Brandstetter,H., Kuhne,A., Bode,W., Huber,R., von der Saal,W., Wirthensohn,K. and Engh,R.A. X-ray structure of active site-inhibited clotting factor Xa. Implications for drug design and substrate recognition J Biol Chem (22-11-1996) 271, 29988-29992. PubMed Europe PubMed DOI S I
Edmunds,J.J. and Rapundalo,S.T. Chapter 6. Thrombin and factor Xa Inhibition Annu Rep Med Chem (1996) 31, 51-60. DOI I
[YEAR:1-11-1996]Plescia,J. and Altieri,D.C. Activation of Mac-1 (CD11b/CD18)-bound factor X by released cathepsin G defines an alternative pathway of leucocyte initiation of coagulation Biochem J (1-11-1996) 319, 873-879. PubMed Europe PubMed PMC EPMC

1995

Lim-Wilby,M.S., Hallenga,K., De Maeyer,M., Lasters,I., Vlasuk,G.P. and Brunck,T.K. NMR structure determination of tick anticoagulant peptide (TAP) Protein Sci (1995) 4, 178-186. PubMed Europe PubMed DOI PMC EPMC S
Matsuzaki,T., Umeyama,H. and Kikumoto,R. Mechanisms of the selective inhibition of thrombin, factor Xa, plasmin and trypsin Pharmacochem Libr (1995) 23, 83-95. DOI S I

1994

[YEAR:5-4-1994]Seymour,J.L., Lindquist,R.N., Dennis,M.S., Moffat,B., Yansura,D., Reilly,D., Wessinger,M.E. and Lazarus,R.A. Ecotin is a potent anticoagulant and reversible tight-binding inhibitor of factor Xa Biochemistry (5-4-1994) 33, 3949-3958. PubMed Europe PubMed

1993

[YEAR:5-8-1993]Padmanabhan,K., Padmanabhan,K.P., Tulinsky,A., Park,C.H., Bode,W., Huber,R., Blankenship,D.T., Cardin,A.D. and Kisiel,W. Structure of human des(1-45) factor Xa at 2.2 A resolution J Mol Biol (5-8-1993) 232, 947-966. PubMed Europe PubMed DOI S

1991

Suzuki,H., Harada,A., Hayashi,Y., Wada,K., Asaka,J., Gotoh,B., Ogasawara,T. and Nagai,Y. Primary structure of the virus activating protease from chick embryo. Its identity with the blood clotting factor Xa FEBS Lett (1991) 283, 281-285. PubMed Europe PubMed DOI

1990

[YEAR:15-10-1990]Neeper,M.P., Waxman,L., Smith,D.E., Schulman,C.A., Sardana,M., Ellis,R.W., Schaffer,L.W., Siegl,P.K. and Vlasuk,G.P. Characterization of recombinant tick anticoagulant peptide. A highly selective inhibitor of blood coagulation factor Xa J Biol Chem (15-10-1990) 265, 17746-17752. PubMed Europe PubMed

1987

[YEAR:5-3-1987]Krishnaswamy,S., Church,W.R., Nesheim,M.E. and Mann,K.G. Activation of human prothrombin by human prothrombinase. Influence of factor Va on the reaction mechanism J Biol Chem (5-3-1987) 262, 3291-3299. PubMed Europe PubMed

1984

Cho,K., Tanaka,T., Cook,R.R., Kisiel,W., Fujikawa,K., Kurachi,K. and Powers,J.C. Active-site mapping of bovine and human blood coagulation serine proteases using synthetic peptide 4-nitroanilide and thio ester substrates Biochemistry (1984) 23, 644-650. PubMed Europe PubMed
[YEAR:10-6-1984]Gitel,S.N., Medina,V.M. and Wessler,S. Inhibition of human activated factor X by antithrombin III and alpha 1-proteinase inhibitor in human plasma J Biol Chem (10-6-1984) 259, 6890-6895. PubMed Europe PubMed
[YEAR:15-5-1984]Jesty,J., Morrison,S.A. and Harpel,P.C. Measurement of human activated factor X-antithrombin complex by an enzyme-linked differential-antibody immunosorbent assay Anal Biochem (15-5-1984) 139, 158-167. PubMed Europe PubMed
[YEAR:1-6-1984]Lijnen,H.R., Uytterhoeven,M. and Collen,D. Inhibition of trypsin-like serine proteinases by tripeptide arginyl and lysyl chloromethylketones Thromb Res (1-6-1984) 34, 431-437. PubMed Europe PubMed I

1983

[YEAR:31-10-1983]Choay,J., Petitou,M., Lormeau,J.C., Sinay,P., Casu,B. and Gatti,G. Structure-activity relationship in heparin: a synthetic pentasaccharide with high affinity for antithrombin III and eliciting high anti-factor Xa activity Biochem Biophys Res Commun (31-10-1983) 116, 492-499. PubMed Europe PubMed
Fuchs,H.E. and Pizzo,S.V. Regulation of factor Xa in vitro in human and mouse plasma and in vivo in mouse. Role of the endothelium and plasma proteinase inhibitors J Clin Invest (1983) 72, 2041-2049. PubMed Europe PubMed DOI PMC EPMC
McMullen,B.A., Fujikawa,K., Kisiel,W., Sasagawa,T., Howald,W.N., Kwa,E.Y. and Weinstein,B. Complete amino acid sequence of the light chain of human blood coagulation factor X: evidence for identification of residue 63 as beta-hydroxyaspartic acid Biochemistry (1983) 22, 2875-2884. PubMed Europe PubMed

1982

[YEAR:4-2-1982]Ellis,V., Scully,M., MacGregor,I. and Kakkar,V. Inhibition of human factor Xa by various plasma protease inhibitors Biochim Biophys Acta (4-2-1982) 701, 24-31. PubMed Europe PubMed

1981

McRae,B.J., Kurachi,K., Heimark,R.L., Fujikawa,K., Davie,E.W. and Powers,J.C. Mapping the active sites of bovine thrombin, factor IXa, factor Xa, factor XIa, factor XIIa, plasma kallikrein, and trypsin with amino acid and peptide thioesters: development of new sensitive substrates Biochemistry (1981) 20, 7196-7206. PubMed Europe PubMed

1980

Enfield,D.L., Ericsson,L.H., Fujikawa,K., Walsh,K.A., Neurath,H. and Titani,K. Amino acid sequence of the light chain of bovine factor X1 (Stuart factor) Biochemistry (1980) 19, 659-667. PubMed Europe PubMed
Jackson,C.M. and Nemerson,Y. Blood coagulation Annu Rev Biochem (1980) 49, 765-811. PubMed Europe PubMed DOI
Robison,D.J., Furie,B., Furie,B.C. and Bing,D.H. Active site of bovine factor Xa. Characterization using substituted benzamidines as competitive inhibitors and affinity-labeling reagents J Biol Chem (1980) 255, 2014-2021. PubMed Europe PubMed I

1979

Davie,E.W., Fujikawa,K., Kurachi,K. and Kisiel,W. The role of serine proteases in the blood coagulation cascade Adv Enzymol Relat Areas Mol Biol (1979) 48, 277-318. PubMed Europe PubMed

1977

Aurell,L., Friberger,P., Karlsson,G. and Claeson,G. A new sensitive and highly specific chromogenic peptide substrate for factor Xa Thromb Res (1977) 11, 595-609. PubMed Europe PubMed
Morita,T., Kato,H., Iwanaga,S., Takada,K., Kimura,T. and Sakakibara,S. New fluorogenic substrates for alpha-thrombin, factor Xa, kallikreins, and urokinase J Biochem (1977) 82, 1495-1498. PubMed Europe PubMed A
Suttie,J.W. and Jackson,C.M. Prothrombin structure, activation, and biosynthesis Physiol Rev (1977) 57, 1-70. PubMed Europe PubMed

1976

Fujikawa,K. and Davie,E.W. Bovine factor X (Stuart factor) Methods Enzymol (1976) 45, 89-95. PubMed Europe PubMed DOI V
Furie,B. and Furie,B.C. Spectral changes in bovine factor X associated with activation by the venom coagulant protein of Vipera russelli J Biol Chem (1976) 251, 6807-6814. PubMed Europe PubMed
Jesty,J. and Nemerson,Y. The activation of bovine coagulation factor X Methods Enzymol (1976) 45, 95-107. PubMed Europe PubMed DOI V
Sturzebecher,J., Markwardt,F. and Walsmann,P. Synthetic inhibitors of serine proteinases. XIV. Inhibition of factor Xa by derivatives of benzamidine Thromb Res (1976) 9, 637-646. PubMed Europe PubMed I

1973

Jameson,G.W., Roberts,D.V., Adams,R.W., Kyle,W.S. and Elmore,D.T. Determination of the operational molarity of solutions of bovine alpha-chymotrypsin, trypsin, thrombin and factor Xa by spectrofluorimetric titration Biochem J (1973) 131, 107-117. PubMed Europe PubMed PMC EPMC I

1972

Jackson,C.M. Characterization of two glycoprotein variants of bovine factor X and demonstration that the factor X zymogen contains two polypeptide chains Biochemistry (1972) 11, 4873-4882. PubMed Europe PubMed
[YEAR:19-12-1972]Titani,K., Hermodson,M.A., Fujikawa,K., Ericsson,L.H., Walsh,K.A., Neurath,H. and Davie,E.W. Bovine factor X1a (activated Stuart factor). Evidence of homology with mammalian serine proteases Biochemistry (19-12-1972) 11, 4899-4903. PubMed Europe PubMed

1962

Esnouf,M.P. and Williams,W.J. The isolation and purification of a bovine-plasma protein which is a substrate for the coagulant fraction of Russell's-viper venom Biochem J (1962) 84, 62-71. PubMed Europe PubMed PMC EPMC

1957

Hougie,C., Barrow,E.M. and Graham,J.B. Stuart clotting defect. I. Segregation of an hereditary hemorrhagic state from the heterogeneous group heretofore called stable factor (SPCA, proconvertin, factor VII) deficiency J Clin Invest (1957) 36, 485-496. PubMed Europe PubMed DOI PMC EPMC M