Reference on EC 3.4.21.6 - coagulation factor Xa and Organism(s) Homo sapiens and UniProt Accession P00742
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AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Franssen, J.; Salemink, I.; Willems, G.M.; Wun, T.C.; Hemker, H.C.; Lindhout, T.
Prothrombinase is protected from inactivation by tissue factor pathway inhibitor: competition between prothrombin and inhibitor
Biochem. J.
323
33-37
1997
Homo sapiens
Kamata, K.; Kawamoto, H.; Honma, T.; Iwama, T.; Kim, S.H.
Structural basis for chemical inhibition of human blood coagulation factor Xa
Proc. Natl. Acad. Sci. USA
95
6630-6635
1998
Homo sapiens (P00742), Homo sapiens
Mao, S.S.; Przysiecki, C.T.; Krueger, J.A.; Cooper, C.M.; Lewis, S.D.; Joyce, J.; Lellis, C.; Garsky, V.M.; Sardana, M.; Shafer, J.A.
Selective inhibition of factor Xa in the prothrombinase complex by the carboxyl-terminal domain of antistasin
J. Biol. Chem.
273
30086-30091
1998
Homo sapiens
Waxman, L.; Smith, D.E.; Arcuri, K.E.; Vlasuk, G.P.
Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa [published erratum appears in Science 1990 Jun 22;248(4962):1473
Science
248
593-596
1990
Homo sapiens
Sinha, U.; Hancock, T.E.; Lin, P.H.; Hollenbach, S.; Wolf, D.L.
Expression, purification, and characterization of inactive human coagulation factor Xa (Asn322Ala419)
Protein Expr. Purif.
3
518-524
1992
Homo sapiens
Scarborough, R.M.
Coagulation factor Xa: the prothrombinase complex as an emerging therapeutic target for small molecule inhibitors
J. Enzyme Inhib.
14
15-25
1998
Homo sapiens
Liang, A.M.; Light, D.R.; Kochanny, M.; Rumennik, G.; Trinh, L.; Lentz, D.; Post, J.; Morser, J.; Snider, M.
Discovery and characterization of a potent and selective non-amidine inhibitor of human factor Xa
Biochem. Pharmacol.
65
1407-1418
2003
Homo sapiens
Rezaie, A.R.; He, X.
Sodium binding site of factor Xa: role of sodium in the prothrombinase complex
Biochemistry
39
1817-1825
2000
Homo sapiens
Monnaie, D.; Arosio, D.; Griffon, N.; Rose, T.; Rezaie, A.R.; Di Cera, E.
Identification of a binding site for quaternary amines in factor Xa
Biochemistry
39
5349-5354
2000
Homo sapiens
Kalafatis, M.; Beck, D.O.
Identification of a binding site for blood coagulation factor Xa on the heavy chain of factor Va. Amino acid residues 323-331 of factor V represent an interactive site for activated factor X
Biochemistry
41
12715-12728
2002
Homo sapiens
Adler, M.; Kochanny, M.J.; Ye, B.; Rumennik, G.; Light, D.R.; Biancalana, S.; Whitlow, M.
Crystal structures of two potent nonamidine inhibitors bound to factor Xa
Biochemistry
41
15514-15523
2002
Homo sapiens (P00742)
Manithody, C.; Yang, L.; Rezaie, A.R.
Role of basic residues of the autolysis loop in the catalytic function of factor Xa
Biochemistry
41
6780-6788
2002
Homo sapiens
Banerjee, M.; Drummond, D.C.; Srivastava, A.; Daleke, D.; Lentz, B.R.
Specificity of soluble phospholipid binding sites on human factor Xa
Biochemistry
41
7751-7762
2002
Homo sapiens
Banerjee, M.; Majumder, R.; Weinreb, G.; Wang, J.; Lentz, B.R.
role of procoagulant lipids in human prothrombin activation. 2. Soluble phosphatidylserine upregulates and directs factor Xa to appropriate peptide bonds in prothrombin
Biochemistry
41
950-957
2002
Homo sapiens
O'Brien, L.A.; Stafford, A.R.; Fredenburgh, J.C.; Weitz, J.I.
Glycosaminoglycans bind factor Xa in a Ca2+-dependent fashion and modulate its catalytic activity
Biochemistry
42
13091-13098
2003
Homo sapiens
Studelska, D.R.; McDowell, L.M.; Adler, M.; O'Connor, R.D.; Mehta, A.K.; Guilford, W.J.; Dallas, J.L.; Arnaiz, D.; Light, D.R.; Schaefer, J.
Conformation of a bound inhibitor of blood coagulant factor Xa
Biochemistry
42
7942-7949
2003
Homo sapiens (P00742), Homo sapiens
Rezaie, A.R.; Yang, L.
Probing the molecular basis of factor Xa specificity by mutagenesis of the serpin, antithrombin
Biochim. Biophys. Acta
1528
167-176
2001
Homo sapiens
Mueller, M.M.; Sperl, S.; Sturzebecher, J.; Bode, W.; Moroder, L.
(R)-3-amidinophenylalanine-derived inhibitors of factor Xa with a novel active-site binding mode
Biol. Chem.
383
1185-1191
2002
Bos taurus, Homo sapiens
Venkateswarlu, D.; Perera, L.; Darden, T.; Pedersen, L.G.
Structure and dynamics of zymogen human blood coagulation factor X
Biophys. J.
82
1190-1206
2002
Homo sapiens (P00742), Homo sapiens
Nishida, H.; Miyazaki, Y.; Kitamura, Y.; Ohashi, M.; Matsusue, T.; Okamoto, A.; Hosaka, Y.; Ohnishi, S.; Mochizuki, H.
Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor
Chem. Pharm. Bull.
49
1237-1244
2001
Homo sapiens
Oliva, M.L.V.; Andrade, S.A.; Juliano, M.A.; Sallai, R.C.; Torquato, R.J.; Sampaio, M.U.; Pott, V.J.; Sampaio, C.A.M.
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.
10
1085-1093
2003
Homo sapiens
Leadley, R.J., Jr.; Chi, L.; Porcari, A.R.
Non-hemostatic activity of coagulation factor Xa: potential implications for various diseases
Curr. Opin. Pharmacol.
1
169-175
2001
Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus, Sus scrofa
Gould, W.R.; Leadley, R.J.
Recent advances in the discovery and development of direct coagulation factor Xa inhibitors
Curr. Pharm. Des.
9
2337-2347
2003
Homo sapiens
Leadley, R.J., Jr.
Coagulation factor Xa inhibition: biological background and rationale
Curr. Top. Med. Chem.
1
151-159
2001
Canis lupus familiaris, Homo sapiens
Heran, C.; Morgan, S.; Kasiewski, C.; Bostwick, J.; Bentley, R.; Klein, S.; Chu, V.; Brown, K.; Colussi, D.; Czekaj, M.; Perrone, M.; Leadley, R.
Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis
Eur. J. Pharmacol.
389
201-207
2000
Homo sapiens, Rattus norvegicus
Hayashi, M.; Matsuo, A.; Nakamoto, H.; Aisaka, K.
Antithrombotic effects of a synthetic inhibitor of activated factor X, JTV-803, in animals
Eur. J. Pharmacol.
412
61-66
2001
Homo sapiens, Rattus norvegicus
Srivastava, A.; Wang, J.; Majumder, R.; Rezaie, A.R.; Stenflo, J.; Esmon, C.T.; Lentz, B.R.
Localization of phosphatidylserine binding sites to structural domains of factor Xa
J. Biol. Chem.
277
1855-1863
2002
Bos taurus, Homo sapiens
Bianchini, E.P.; Louvain, V.B.; Marque, P.E.; Juliano, M.A.; Juliano, L.; Le Bonniec, B.F.
Mapping of the catalytic groove preferences of factor Xa reveals an inadequate selectivity for its macromolecule substrates
J. Biol. Chem.
277
20527-20534
2002
Homo sapiens
Buddai, S.K.; Toulokhonova, L.; Bergum, P.W.; Vlasuk, G.P.; Krishnaswamy, S.
Nematode anticoagulant protein c2 reveals a site on factor Xa that is important for macromolecular substrate binding to human prothrombinase
J. Biol. Chem.
277
26689-26698
2002
Homo sapiens
Harrison, L.M.; Nerlinger, A.; Bungiro, R.D.; Cordova, J.L.; Kuzmic, P.; Cappello, M.
Molecular characterization of Ancylostoma inhibitors of coagulation factor Xa. Hookworm anticoagulant activity in vitro predicts parasite bloodfeeding in vivo
J. Biol. Chem.
277
6223-6229
2002
Homo sapiens
Kalafatis, M.; Beck, D.O.; Mann, K.G.
Structural requirements for expression of factor Va activity
J. Biol. Chem.
278
33550-33561
2003
Homo sapiens
Brufatto, N.; 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.
278
6755-6764
2003
Homo sapiens
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.; Mikol, V.
Crystal structures of human factor Xa complexed with potent inhibitors
J. Med. Chem.
43
3226-3232
2000
Homo sapiens (P00742), Homo sapiens
Verner, E.; Katz, B.A.; Spencer, J.R.; Allen, D.; Hataye, J.; Hruzewicz, W.; Hui, H.C.; Kolesnikov, A.; Li, Y.; Luong, C.; Martelli, A.; Radika, K.; Rai, R.; She, M.; Shrader, W.; Sprengeler, P.A.; Trapp, S.; Wang, J.; Young, W.B.; Mackman, R.L.
Development of serine protease inhibitors displaying a multicentered short 2.3 ANG hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa
J. Med. Chem.
44
2753-2771
2001
Homo sapiens
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.; 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.
44
566-578
2001
Homo sapiens
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.; Mikol, V.
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand
J. Med. Chem.
46
681-684
2003
Homo sapiens, Rattus norvegicus
Li, Y.; Spencer, F.A.; Ball, S.; Becker, R.C.
Inhibition of platelet-dependent prothrombinase activity and thrombin generation by glycoprotein IIb/IIIa receptor-directed antagonists: potential contributing mechanism of benefit in acute coronary syndromes
J. Thromb. Thrombolysis
10
69-76
2000
Homo sapiens
Lorentsen, R.H.; Moller, C.H.; Etzerodt, M.; Thogersen, H.C.; Holtet, T.L.
Substrate turnover and inhibitor binding as selection parameters in directed evolution of blood coagulation factor Xa
Org. Biomol. Chem.
1
1657-1663
2003
Homo sapiens
Nar, H.; Bauer, M.; Schmid, A.; Stassen, J.M.; Wienen, W.; Priepke, H.W.M.; Kauffmann, I.K.; Ries, U.J.; Hauel, N.H.
Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors
Structure
9
29-37
2001
Homo sapiens (P00742), Homo sapiens
Chu, V.; Brown, K.; Colussi, D.; Gao, J.; Bostwick, J.; Kasiewski, C.; Bentley, R.; Morgan, S.; Guertin, K.; Pauls, H.W.; Gong, Y.; Zulli, A.; Perrone, M.H.; Dunwiddie, C.T.; Leadley, R.J.
Pharmacological characterization of a novel factor Xa inhibitor, FXV673
Thromb. Res.
103
309-324
2001
Canis lupus familiaris, Oryctolagus cuniculus, Homo sapiens
Chu, V.; Brown, K.; Colussi, D.; Choi, Y.M.; Green, D.; Pauls, H.W.; Spada, A.P.; Perrone, M.H.; Leadley, R.J.; Dunwiddie, C.T.
In vitro characterization of a novel factor Xa inhibitor, RPR 130737
Thromb. Res.
99
71-82
2000
Homo sapiens
Gould, W.R.; Cladera, E.; Harris, M.S.; Zhang, E.; Narasimhan, L.; Thorn, J.M.; Leadley, R.J.
Co-crystal structure and inhibition of factor Xa by PD0313052 identifies structurally stabilized active site residues of factor Xa and prothrombinase
Biochemistry
44
9280-9289
2005
Homo sapiens
Bianchini, E.P.; Pike, R.N.; Le Bonniec, B.F.
The elusive role of the potential factor X cation-binding exosite-1 in substrate and inhibitor interactions
J. Biol. Chem.
279
3671-3679
2004
Homo sapiens
Orcutt, S.J.; Krishnaswamy, S.
Binding of substrate in two conformations to human prothrombinase drives consecutive cleavage at two sites in prothrombin
J. Biol. Chem.
279
54927-54936
2004
Homo sapiens
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.; Edmunds, J.J.
Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa
J. Med. Chem.
47
4089-4099
2004
Homo sapiens
Whinna, H.C.; Lesesky, E.B.; Monroe, D.M.; High, K.A.; Larson, P.J.; Church, F.C.
Role of the gamma-carboxyglutamic acid domain of activated factor X in the presence of calcium during inhibition by antithrombin-heparin
J. Thromb. Haemost.
2
1127-1134
2004
Homo sapiens
Ieko, M.; Tarumi, T.; Takeda, M.; Naito, S.; Nakabayashi, T.; 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.
2
612-618
2004
Homo sapiens
Tanaka, M.; Arai, H.; Liu, N.; Nogaki, F.; Nomura, K.; Kasuno, K.; Oida, E.; Kita, T.; Ono, T.
Role of coagulation factor Xa and protease-activated receptor 2 in human mesangial cell proliferation
Kidney Int.
67
2123-2133
2005
Homo sapiens
Dennis, M.W.; Downey, C.; Brufatto, N.; Nesheim, M.E.; Stevenson, K.; Toh, C.H.
Prothrombinase enhancement through quantitative and qualitative changes affecting very low density lipoprotein in complex with C-reactive protein
Thromb. Haemost.
91
522-530
2004
Homo sapiens
Daubie, V.; Cauwenberghs, S.; Senden, N.H.; Pochet, R.; Lindhout, T.; Buurman, W.A.; Heemskerk, J.W.
Factor Xa and thrombin evoke additive calcium and proinflammatory responses in endothelial cells subjected to coagulation
Biochim. Biophys. Acta
1763
860-869
2006
Bos taurus, Homo sapiens
Fevig, J.M.; Cacciola, J.; Buriak, J.; Rossi, K.A.; Knabb, R.M.; Luettgen, J.M.; Wong, P.C.; Bai, S.A.; Wexler, R.R.; 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.
16
3755-3760
2006
Homo sapiens
Pinto, D.J.; Galemmo, R.A.; 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.; Lam, P.Y.
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
Bioorg. Med. Chem. Lett.
16
5584-5589
2006
Homo sapiens
Nagata, T.; Yoshino, T.; Haginoya, N.; Yoshikawa, K.; Isobe, Y.; Furugohri, T.; Kanno, H.
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors
Bioorg. Med. Chem. Lett.
17
4683-4688
2007
Homo sapiens
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.; Quan, M.L.
Sulfonamidolactam inhibitors of coagulation factor Xa
Bioorg. Med. Chem. Lett.
18
2428-2433
2008
Homo sapiens
Silva, F.P.; Antunes, O.A.; de Alencastro, R.B.; De Simone, S.G.
The Na+ binding channel of human coagulation proteases: Novel insights on the structure and allosteric modulation revealed by molecular surface analysis
Biophys. Chem.
119
282-294
2006
Homo sapiens
Panteleev, M.A.; Ovanesov, M.V.; Kireev, D.A.; Shibeko, A.M.; Sinauridze, E.I.; Ananyeva, N.M.; Butylin, A.A.; Saenko, E.L.; Ataullakhanov, F.I.
Spatial propagation and localization of blood coagulation are regulated by intrinsic and protein C pathways, respectively
Biophys. J.
90
1489-1500
2006
Homo sapiens
Khrenov, A.V.; Ananyeva, N.M.; Saenko, E.L.
Role of the B domain in proteolytic inactivation of activated coagulation factor VIII by activated protein C and activated factor X
Blood Coagul. Fibrinolysis
17
379-388
2006
Homo sapiens
Faure, G.; Gowda, V.T.; Maroun, R.C.
Characterization of a human coagulation factor Xa-binding site on Viperidae snake venom phospholipases A2 by affinity binding studies and molecular bioinformatics
BMC Struct. Biol.
7
82
2007
Homo sapiens (P00742), Homo sapiens
Borensztajn, K.S.; Bijlsma, M.F.; Groot, A.P.; Brueggemann, L.W.; Versteeg, H.H.; Reitsma, P.H.; Peppelenbosch, M.P.; Spek, C.A.
Coagulation factor Xa drives tumor cells into apoptosis through BH3-only protein Bim up-regulation
Exp. Cell Res.
313
2622-2633
2007
Homo sapiens
Norstrom, E.A.; Tran, S.; Steen, M.; Dahlbaeck, B.
Effects of factor Xa and protein S on the individual activated protein C-mediated cleavages of coagulation factor Va
J. Biol. Chem.
281
31486-31494
2006
Homo sapiens
Izaguirre, G.; Swanson, R.; Raja, S.M.; Rezaie, A.R.; Olson, S.T.
Mechanism by which exosites promote the inhibition of blood coagulation proteases by heparin-activated antithrombin
J. Biol. Chem.
282
33609-33622
2007
Homo sapiens
Gould, W.R.; McClanahan, T.B.; Welch, K.M.; Baxi, S.M.; Saiya-Cork, K.; Chi, L.; Johnson, T.R.; Leadley, R.J.
Inhibitors of blood coagulation factors Xa and IIa synergize to reduce thrombus weight and thrombin generation in vivo and in vitro
J. Thromb. Haemost.
4
834-841
2006
Homo sapiens
Calatzis, A.; Peetz, D.; Haas, S.; Spannagl, M.; Rudin, K.; Wilmer, M.
Prothrombinase-induced clotting time assay for determination of the anticoagulant effects of unfractionated and low-molecular-weight heparins, fondaparinux, and thrombin inhibitors
Am. J. Clin. Pathol.
130
446-454
2008
Homo sapiens
Fiore, M.M.; Mackie, I.J.
Dual effect of platelet factor 4 on the activities of factor Xa
Biochem. Biophys. Res. Commun.
379
1072-1075
2009
Homo sapiens
Yang, L.; Manithody, C.; Qureshi, S.H.; Rezaie, A.R.
Factor Va alters the conformation of the Na+-binding loop of factor Xa in the prothrombinase complex
Biochemistry
47
5976-5985
2008
Homo sapiens
Barhoover, M.A.; Orban, T.; Beck, D.O.; Bukys, M.A.; Kalafatis, M.
Contribution of amino acid region 334-335 from factor Va heavy chain to the catalytic efficiency of prothrombinase
Biochemistry
47
6840-6850
2008
Homo sapiens
Hirbawi, J.; Bukys, M.A.; Barhoover, M.A.; Erdogan, E.; Kalafatis, M.
Role of the acidic hirudin-like COOH-terminal amino acid region of factor Va heavy chain in the enhanced function of prothrombinase
Biochemistry
47
7963-7974
2008
Homo sapiens
Sun, W.; Eriksson, A.S.; Schedin-Weiss, S.
Heparin enhances the inhibition of factor Xa by protein C inhibitor in the presence but not in the absence of Ca2+
Biochemistry
48
1094-1098
2009
Homo sapiens
Joo, S.S.; Won, T.J.; Kim, J.S.; Yoo, Y.M.; Tak, E.S.; Park, S.Y.; Park, H.Y.; Hwang, K.W.; Park, S.C.; Lee, D.I.
Inhibition of coagulation activation and inflammation by a novel Factor Xa inhibitor synthesized from the earthworm Eisenia andrei
Biol. Pharm. Bull.
32
253-258
2009
Homo sapiens
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.; 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.
18
4118-4123
2008
Homo sapiens
Nagata, T.; Nagamochi, M.; Kobayashi, S.; Komoriya, S.; Yoshino, T.; Kanno, H.
Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors
Bioorg. Med. Chem. Lett.
18
4587-4592
2008
Homo sapiens, Rattus norvegicus
Qiao, J.X.; King, S.R.; He, K.; Wong, P.C.; Rendina, A.R.; Luettgen, J.M.; Xin, B.; Knabb, R.M.; Wexler, R.R.; Lam, P.Y.
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties
Bioorg. Med. Chem. Lett.
19
462-468
2009
Homo sapiens
Imaeda, Y.; Kawamoto, T.; Tobisu, M.; Konishi, N.; Hiroe, K.; Kawamura, M.; Tanaka, T.; Kubo, K.
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors
Bioorg. Med. Chem.
16
3125-3140
2008
Macaca fascicularis, Homo sapiens
Nagata, T.; Yoshino, T.; Haginoya, N.; Yoshikawa, K.; Nagamochi, M.; Kobayashi, S.; Komoriya, S.; Yokomizo, A.; Muto, R.; Yamaguchi, M.; Osanai, K.; Suzuki, M.; Kanno, H.
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa
Bioorg. Med. Chem.
17
1193-1206
2009
Homo sapiens
Chattopadhyay, R.; Iacob, R.; Sen, S.; Majumder, R.; Tomer, K.B.; Lentz, B.R.
Functional and structural characterization of factor Xa dimer in solution
Biophys. J.
96
974-986
2009
Homo sapiens
Singh, N.; Briggs, J.M.
Molecular dynamics simulations of Factor Xa: insight into conformational transition of its binding subsites
Biopolymers
89
1104-1113
2008
Homo sapiens (P00742), Homo sapiens
Coggin, M.H.; Srapionian, R.M.; Brecher, A.S.; Galoyan, A.A.
Comparative effects of atrial polypeptide and neurohormone C on the interaction of factor Xa with antithrombin III
Blood Coagul. Fibrinolysis
19
645-651
2008
Homo sapiens
Majumder, R.; Quinn-Allen, M.A.; Kane, W.H.; Lentz, B.R.
A phosphatidylserine binding site in factor Va C1 domain regulates both assembly and activity of the prothrombinase complex
Blood
112
2795-2802
2008
Homo sapiens
Noguchi, T.; Tanaka, N.; Nishimata, T.; Goto, R.; Hayakawa, M.; Sugidachi, A.; Ogawa, T.; Asai, F.; Fujimoto, K.
Cinnamyl derivatives: synthesis and factor Xa (FXa) inhibitory activities
Chem. Pharm. Bull.
56
758-770
2008
Homo sapiens
Noguchi, T.; Tanaka, N.; Nishimata, T.; Goto, R.; Hayakawa, M.; Sugidachi, A.; Ogawa, T.; Niitsu, Y.; Asai, F.; Ishizuka, T.; Fujimoto, K.
Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives
Chem. Pharm. Bull.
57
22-33
2009
Canis lupus familiaris, Homo sapiens
Bhattacharjee, G.; Ahamed, J.; Pawlinski, R.; Liu, C.; Mackman, N.; Ruf, W.; Edgington, T.S.
Factor Xa binding to annexin 2 mediates signal transduction via protease-activated receptor 1
Circ. Res.
102
457-464
2008
Homo sapiens
Abel, R.; Young, T.; Farid, R.; Berne, B.J.; Friesner, R.A.
Role of the active-site solvent in the thermodynamics of factor Xa ligand binding
J. Am. Chem. Soc.
130
2817-2831
2008
Homo sapiens
Hsu, H.J.; Tsai, K.C.; Sun, Y.K.; Chang, H.J.; Huang, Y.J.; Yu, H.M.; Lin, C.H.; Mao, S.S.; Yang, A.S.
Factor Xa active site substrate specificity with substrate phage display and computational molecular modeling
J. Biol. Chem.
283
12343-12353
2008
Bos taurus, Homo sapiens
Toso, R.; Zhu, H.; Camire, R.M.
The conformational switch from the factor X zymogen to protease state mediates exosite expression and prothrombinase assembly
J. Biol. Chem.
283
18627-18635
2008
Homo sapiens
Steen, M.; Tran, S.; Autin, L.; Villoutreix, B.O.; Tholander, A.L.; Dahlbaeck, B.
Mapping of the factor Xa binding site on factor Va by site-directed mutagenesis
J. Biol. Chem.
283
20805-20812
2008
Homo sapiens
Huang, X.; Swanson, R.; Broze, G.J.; Olson, S.T.
Kinetic characterization of the protein Z-dependent protease inhibitor reaction with blood coagulation factor Xa
J. Biol. Chem.
283
29770-29783
2008
Homo sapiens
Kamath, P.; Krishnaswamy, S.
Fate of membrane-bound reactants and products during the activation of human prothrombin by prothrombinase
J. Biol. Chem.
283
30164-30173
2008
Homo sapiens
Yegneswaran, S.; Hackeng, T.M.; Dawson, P.E.; Griffin, J.H.
The thrombin-sensitive region of protein S mediates phospholipid-dependent interaction with factor Xa
J. Biol. Chem.
283
33046-33052
2008
Homo sapiens
Izaguirre, G.; Rezaie, A.R.; Olson, S.T.
Engineering functional antithrombin exosites in alpha1-proteinase inhibitor that specifically promote the inhibition of factor Xa and factor IXa
J. Biol. Chem.
284
1550-1558
2009
Homo sapiens
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.; Toomey, J.R.
Antithrombotic potential of GW813893: a novel, orally active, active-site directed factor Xa inhibitor
J. Cardiovasc. Pharmacol.
52
66-71
2008
Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus
Rohde, G.
Determination of rivaroxaban - a novel, oral, direct Factor Xa inhibitor - in human plasma by high-performance liquid chromatography-tandem mass spectrometry
J. Chromatogr. B
872
43-50
2008
Homo sapiens
Imaeda, Y.; Kuroita, T.; Sakamoto, H.; Kawamoto, T.; Tobisu, M.; Konishi, N.; Hiroe, K.; Kawamura, M.; Tanaka, T.; Kubo, K.
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors
J. Med. Chem.
51
3422-3436
2008
Macaca fascicularis, Homo sapiens, Rattus norvegicus
Furugohri, T.; Isobe, K.; Honda, Y.; Kamisato-Matsumoto, C.; Sugiyama, N.; Nagahara, T.; Morishima, Y.; Shibano, T.
DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles
J. Thromb. Haemost.
6
1542-1549
2008
Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus
Mueller, J.; Freitag, D.; Mayer, G.; Poetzsch, B.
Anticoagulant characteristics of HD1-22, a bivalent aptamer that specifically inhibits thrombin and prothrombinase
J. Thromb. Haemost.
6
2105-2112
2008
Homo sapiens
Wong, P.C.; Crain, E.J.; Xin, B.; Wexler, R.R.; Lam, P.Y.; Pinto, D.J.; Luettgen, J.M.; Knabb, R.M.
Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies
J. Thromb. Haemost.
6
820-829
2008
Canis lupus familiaris, Oryctolagus cuniculus, Homo sapiens, Rattus norvegicus
Turpie, A.G.; Bauer, K.A.; Davidson, B.L.; Fisher, W.D.; Gent, M.; Huo, M.H.; Sinha, U.; Gretler, D.D.; Gretler, D.D.
A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT)
Thromb. Haemost.
101
68-76
2009
Homo sapiens
Bukys, M.A.; Orban, T.; Kim, P.Y.; Nesheim, M.E.; Kalafatis, M.
The interaction of fragment 1 of prothrombin with the membrane surface is a prerequisite for optimum expression of factor Va cofactor activity within prothrombinase
Thromb. Haemost.
99
511-522
2008
Homo sapiens
Borensztajn, K.; Bijlsma, M.F.; Reitsma, P.H.; Peppelenbosch, M.P.; Spek, C.A.
Coagulation Factor Xa inhibits cancer cell migration via protease-activated receptor-1 activation
Thromb. Res.
124
219-225
2009
Homo sapiens
Rauch, U.
Rivaroxaban - once daily, oral, direct factor Xa inhibition compared with vitamin K antagonism for prevention of stroke and embolism trial in atrial fibrillation: rationale and design of the ROCKET AF study
Am. Heart J.
159
340-347.e1
2010
Homo sapiens
Batista, I.F.; Ramos, O.H.; Ventura, J.S.; Junqueira-de-Azevedo, I.L.; Ho, P.L.; Chudzinski-Tavassi, A.M.
A new factor Xa inhibitor from Amblyomma cajennense with a unique domain composition
Arch. Biochem. Biophys.
493
151-156
2010
Homo sapiens
Perzborn, E.; Roehrig, S.; Straub, A.; Kubitza, D.; Mueck, W.; Laux, V.
Rivaroxaban: a new oral factor Xa inhibitor
Arterioscler. Thromb. Vasc. Biol.
30
376-381
2010
Homo sapiens
Quan, M.L.; Pinto, D.J.; Rossi, K.A.; Sheriff, S.; Alexander, R.S.; Amparo, E.; Kish, K.; Knabb, R.M.; Luettgen, J.M.; Morin, P.; Smallwood, A.; Woerner, F.J.; Wexler, R.R.
Phenyltriazolinones as potent factor Xa inhibitors
Bioorg. Med. Chem. Lett.
20
1373-1377
2010
Homo sapiens
Zhao, X.; Sun, P.; Zhou, Y.; Liu, Y.; Zhang, H.; Mueck, W.; Kubitza, D.; Bauer, R.J.; Zhang, H.; Cui, Y.
Safety, pharmacokinetics and pharmacodynamics of single/multiple doses of the oral, direct factor Xa inhibitor rivaroxaban in healthy Chinese subjects
Br. J. Clin. Pharmacol.
68
77-88
2009
Homo sapiens
Zikria, J.C.; Ansell, J.
Oral anticoagulation with factor Xa and thrombin inhibitors: on the threshold of change
Curr. Opin. Hematol.
16
347-356
2009
Homo sapiens
Lang, D.; Freudenberger, C.; Weinz, C.
In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans
Drug Metab. Dispos.
37
1046-1055
2009
Canis lupus familiaris, Homo sapiens, Rattus norvegicus
Weinz, C.; Schwarz, T.; Kubitza, D.; Mueck, W.; Lang, D.
Metabolism and excretion of rivaroxaban, an oral, direct factor Xa inhibitor, in rats, dogs, and humans
Drug Metab. Dispos.
37
1056-1064
2009
Canis lupus familiaris, Homo sapiens, Rattus norvegicus
Wang, L.; Zhang, D.; Raghavan, N.; Yao, M.; Ma, L.; Frost, C.E.; Frost, C.A.; Maxwell, B.D.; Chen, S.Y.; He, K.; Goosen, T.C.; Humphreys, W.G.; Grossman, S.J.
In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies
Drug Metab. Dispos.
38
448-458
2010
Homo sapiens
de Candia, M.; Lopopolo, G.; Altomare, C.
Novel factor Xa inhibitors: a patent review
Expert Opin. Ther. Pat.
19
1535-1580
2009
Homo sapiens
Gan, W.; Deng, L.; Yang, C.; He, Q.; Hu, J.; Yin, H.; Jin, X.; Lu, C.; Wu, Y.; Peng, L.
An anticoagulant peptide from the human hookworm, Ancylostoma duodenale that inhibits coagulation factors Xa and XIa
FEBS Lett.
583
1976-1980
2009
Homo sapiens
Gettins, P.G.; Olson, S.T.
Activation of antithrombin as a factor IXa and Xa inhibitor involves mitigation of repression rather than positive enhancement
FEBS Lett.
583
3397-3400
2009
Homo sapiens
Perzborn, E.
Factor Xa inhibitors - new anticoagulants for secondary haemostasis
Hamostaseologie
29
260-267
2009
Homo sapiens
Imberti, D.; DallAsta, C.; Pierfranceschi, M.G.
Oral factor Xa inhibitors for thromboprophylaxis in major orthopedic surgery: a review
Intern. Emerg. Med.
4
471-477
2009
Homo sapiens
Bradford, H.N.; Micucci, J.A.; Krishnaswamy, S.
Regulated cleavage of prothrombin by prothrombinase: repositioning a cleavage site reveals the unique kinetic behavior of the action of prothrombinase on its compound substrate
J. Biol. Chem.
285
328-338
2010
Homo sapiens
Buddai, S.K.; Layzer, J.M.; Lu, G.; Rusconi, C.P.; Sullenger, B.A.; Monroe, D.M.; Krishnaswamy, S.
An anticoagulant RNA aptamer that inhibits proteinase-cofactor interactions within prothrombinase
J. Biol. Chem.
285
5212-5223
2010
Homo sapiens
Gomes, A.M.; Kozlowski, E.O.; Pomin, V.H.; de Barros, C.M.; Zaganeli, J.L.; Pavao, M.S.
Unique extracellular matrix heparan sulfate from the bivalve Nodipecten nodosus (Linnaeus, 1758) safely inhibits arterial thrombosis after photochemically induced endothelial lesion
J. Biol. Chem.
285
7312-7323
2010
Homo sapiens
Steffel, J.; Luescher, T.F.
Novel anticoagulants in clinical development: focus on factor Xa and direct thrombin inhibitors
J. Cardiovasc. Med.
10
616-623
2009
Homo sapiens
de Candia, M.; Liantonio, F.; Carotti, A.; De Cristofaro, R.; Altomare, C.
Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation
J. Med. Chem.
52
1018-1028
2009
Homo sapiens
Chandrasekaran, V.; Lee, C.J.; Lin, P.; Duke, R.E.; Pedersen, L.G.
A computational modeling and molecular dynamics study of the Michaelis complex of human protein Z-dependent protease inhibitor (ZPI) and factor Xa (FXa)
J. Mol. Model.
15
897-911
2009
Homo sapiens
Veyrat-Follet, C.; Vivier, N.; Trellu, M.; Dubruc, C.; Sanderink, G.J.
The pharmacokinetics of idraparinux, a long-acting indirect factor Xa inhibitor: population pharmacokinetic analysis from phase III clinical trials
J. Thromb. Haemost.
7
559-565
2009
Homo sapiens
Roser-Jones, C.; Becker, R.C.
Apixaban: an emerging oral factor Xa inhibitor
J. Thromb. Thrombolysis
29
141-146
2010
Homo sapiens
Chafa, O.; Tagzirt, M.; Tapon-Bretaudiere, J.; Reghis, A.; Fischer, A.M.; LeBonniec, B.F.
Characterization of a homozygous Gly11Val mutation in the Gla domain of coagulation factor X
Thromb. Res.
124
144-148
2009
Homo sapiens
Borensztajn, K.; Peppelenbosch, M.P.; Spek, C.A.
Coagulation Factor Xa inhibits cancer cell migration via LIMK1-mediated cofilin inactivation
Thromb. Res.
125
e323-e328
2010
Homo sapiens
Fadeeva, O.A.; Panteleev, M.A.; Karamzin, S.S.; Balandina, A.N.; Smirnov, I.V.; Ataullakhanov, F.I.
Thromboplastin immobilized on polystyrene surface exhibits kinetic characteristics close to those for the native protein and activates in vitro blood coagulation similarly to thromboplastin on fibroblasts
Biochemistry (Moscow)
75
734-743
2010
Homo sapiens
Hirbawi, J.; Vaughn, J.L.; Bukys, M.A.; Vos, H.L.; Kalafatis, M.
Contribution of amino acid region 659-663 of Factor Va heavy chain to the activity of factor Xa within prothrombinase
Biochemistry
49
8520-8534
2010
Homo sapiens
Young, R.J.; Adams, C.; Blows, M.; Brown, D.; Burns-Kurtis, C.L.; Chan, C.; Chaudry, L.; Convery, M.A.; Davies, D.E.; Exall, A.M.; Foster, G.; Harling, J.D.; Hortense, E.; Irvine, S.; Irving, W.R.; Jackson, S.; Kleanthous, S.; Pateman, A.J.; Patikis, A.N.; Roethka, T.J.; Senger, S.; Stelman, G.J.; Toomey, J.R.
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs
Bioorg. Med. Chem. Lett.
21
1582-1587
2011
Homo sapiens
Watson, N.S.; Adams, C.; Belton, D.; Brown, D.; Burns-Kurtis, C.L.; Chaudry, L.; Chan, C.; Convery, M.A.; Davies, D.E.; Exall, A.M.; Harling, J.D.; Irvine, S.; Irving, W.R.; Kleanthous, S.; McLay, I.M.; Pateman, A.J.; Patikis, A.N.; Roethke, T.J.; Senger, S.; Stelman, G.J.; Toomey, J.R.; West, R.I.; Whittaker, C.
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs
Bioorg. Med. Chem. Lett.
21
1588-1592
2011
Homo sapiens
Yoshikawa, K.; Yoshino, T.; Yokomizo, Y.; Uoto, K.; Naito, H.; Kawakami, K.; Mochizuki, A.; Nagata, T.; Suzuki, M.; Kanno, H.; Takemura, M.; Ohta, T.
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
Bioorg. Med. Chem. Lett.
21
2133-2140
2011
Homo sapiens
Lee, C.J.; Wu, S.; Eun, C.; Pedersen, L.G.
A revisit to the one form kinetic model of prothrombinase
Biophys. Chem.
149
28-33
2010
Homo sapiens
Kroh, H.K.; Panizzi, P.; Tchaikovski, S.; Baird, T.R.; Wei, N.; Krishnaswamy, S.; Tans, G.; Rosing, J.; Furie, B.; Furie, B.C.; Bock, P.E.
Active site-labeled prothrombin inhibits prothrombinase in vitro and thrombosis in vivo
J. Biol. Chem.
286
23345-23356
2011
Homo sapiens, Mus musculus
Pinto, D.; Smallheer, J.; Cheney, D.; Knabb, R.; Wexler, R.
Factor Xa inhibitors: Next-generation antithrombotic agents
J. Med. Chem.
53
6243-6274
2010
Homo sapiens
Al-Horani, R.A.; Liang, A.; Desai, U.R.
Designing nonsaccharide, allosteric activators of antithrombin for accelerated inhibition of factor Xa
J. Med. Chem.
54
6125-6138
2011
Homo sapiens
Kim, P.Y.; Nesheim, M.E.
Down regulation of prothrombinase by activated protein C during prothrombin activation
Thromb. Haemost.
104
61-70
2010
Homo sapiens
Koklic, T.; Majumder, R.; Lentz, B.R.
Ca2+ switches the effect of PS-containing membranes on Factor Xa from activating to inhibiting: implications for initiation of blood coagulation
Biochem. J.
462
591-601
2014
Homo sapiens
Griffiths, A.E.; Wintermute, J.; Newell-Caito, J.L.; Fay, P.J.
Residues flanking scissile bonds in Factor VIII modulate rates of cleavage and proteolytic activation catalyzed by Factor Xa
Biochemistry
52
8060-8068
2013
Homo sapiens
Ishihara, T.; Koga, Y.; Iwatsuki, Y.; Hirayama, F.
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system
Bioorg. Med. Chem.
23
277-289
2015
Homo sapiens
Boehm, A.; Floesser, A.; Ermler, S.; Fender, A.C.; Lueth, A.; Kleuser, B.; Schroer, K.; Rauch, B.H.
Factor-Xa-induced mitogenesis and migration require sphingosine kinase activity and S1P formation in human vascular smooth muscle cells
Cardiovasc. Res.
99
505-513
2013
Homo sapiens
Bukowska, A.; Zacharias, I.; Weinert, S.; Skopp, K.; Hartmann, C.; Huth, C.; Goette, A.
Coagulation factor Xa induces an inflammatory signalling by activation of protease-activated receptors in human atrial tissue
Eur. J. Pharmacol.
718
114-123
2013
Homo sapiens
Hollborn, M.; Kohen, L.; Werschnik, C.; Tietz, L.; Wiedemann, P.; Bringmann, A.
Activated blood coagulation factor X (FXa) induces angiogenic growth factor expression in human retinal pigment epithelial cells
Invest. Ophthalmol. Vis. Sci.
53
5930-5939
2012
Homo sapiens
Nguyen, C.N.; Cruz, A.; Gilson, M.K.; Kurtzman, T.
Thermodynamics of Water in an Enzyme Active Site: Grid-based hydration analysis of coagulation factor Xa
J. Chem. Theory Comput.
10
2769-2780
2014
Homo sapiens
Al-Sallami, H.S.; Medlicott, N.J.
Investigation of an anti-activated factor X (anti-Xa) assay for the quantification of enoxaparin in human plasma
J. Pharm. Pharmacol.
67
209-214
2015
Homo sapiens
Henry, B.L.; Desai, U.R.
Sulfated low molecular weight lignins, allosteric inhibitors of coagulation proteinases via the heparin binding site, significantly alter the active site of thrombin and factor Xa compared to heparin
Thromb. Res.
134
1123-1129
2014
Homo sapiens
Koklic, T.; Chattopadhyay, R.; Majumder, R.; Lentz, B.R.
Factor Xa dimerization competes with prothrombinase complex formation on platelet-like membrane surfaces
Biochem. J.
467
37-46
2015
Bos taurus, Homo sapiens
Dhar, A.; Sadiq, F.; Anstee, Q.M.; Levene, A.P.; Goldin, R.D.; Thursz, M.R.
Thrombin and factor Xa link the coagulation system with liver fibrosis
BMC Gastroenterol.
18
60
2018
Homo sapiens, Mus musculus
Yang, J.; Su, G.; Ren, Y.; Chen, Y.
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors
Eur. J. Med. Chem.
101
41-51
2015
Homo sapiens
Ilin, I.; Lipets, E.; Sulimov, A.; Kutov, D.; Shikhaliev, K.; Potapov, A.; Krysin, M.; Zubkov, F.; Sapronova, L.; Ataullakhanov, F.; Sulimov, V.
New factor Xa inhibitors based on 1,2,3,4-tetrahydroquinoline developed by molecular modelling
J. Mol. Graph. Model.
89
215-224
2019
Homo sapiens (P00742)
Pryzdial, E.L.; Meixner, S.C.; Talbot, K.; Eltringham-Smith, L.J.; Baylis, J.R.; Lee, F.M.; Kastrup, C.J.; Sheffield, W.P.
Thrombolysis by chemically modified coagulation factor Xa
J. Thromb. Haemost.
14
1844-1854
2016
Homo sapiens
Verhoef, D.; Visscher, K.M.; Vosmeer, C.R.; Cheung, K.L.; Reitsma, P.H.; Geerke, D.P.; Bos, M.H.A.
Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors
Nat. Commun.
8
528
2017
Homo sapiens
Gera, O.; Bushi, D.; Ben Shimon, M.; Artan-Furman, A.; Harnof, S.; Maggio, N.; Dori, A.; Chapman, J.; Shavit-Stein, E.
Local regulation of thrombin activity by factor Xa in peripheral nerve Schwann cells
Neuroscience
371
445-454
2018
Homo sapiens, Mus musculus
