Crystal structures of human factor Xa complexed with potent inhibitors

Journal of Medicinal Chemistry

Volumn 43, Issue 17, 2000, Pages 3226-3232

  Maignan, S ^a   Guilloteau, J P ^a   Pouzieux, S ^a   Choi Sledeski, Y M ^a   Becker, M R ^b   Klein, S I ^b   Ewing, W R ^b   Pauls, H W ^b   Spada, A P ^b   Mikol, V ^a  

^a SANOFI   (France)

^b Aventis Pharmaceuticals   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ASPARTIC ACID; BENZAMIDINE DERIVATIVE; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; LIGAND; SERINE PROTEINASE; SERINE PROTEINASE INHIBITOR; THROMBIN;

ARTICLE; BLOOD CLOTTING; CELL SPECIFICITY; COVALENT BOND; CRYSTAL STRUCTURE; CRYSTALLIZATION; DRUG SCREENING; HEMOSTASIS; HYDROGEN BOND; MOLECULAR INTERACTION; PROTEIN BINDING; PROTEIN PROTEIN INTERACTION;

BENZAMIDINES; CRYSTALLOGRAPHY, X-RAY; FACTOR XA; FIBRINOLYTIC AGENTS; HUMANS; LIGANDS; MODELS, MOLECULAR; PROTEIN BINDING; PROTEIN CONFORMATION; SERINE PROTEINASE INHIBITORS; TRYPSIN;

EID: 0034710722     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000940u     Document Type: Article

References (20)

1. Role of thrombin compared with factor Xa in the procoagulant activity of whole blood clots
2. Thrombin and factor Xa inhibitors
3. Low molecular weight heparins
4. Structure of human des(1-45) factor Xa at 2.2 Å
5. X-ray structure of the active site-inhibited clotting factor Xa
6. Structural basis for chemical inhibition of human blood coagulation factor Xa
7. Crystal structures of thrombin and thrombin complexes as a framework for antithrombotic drug design
8. Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin
9. Crystal structures of factor Xa specific inhibitors in complex with trypsin: Structural grounds for inhibition of factor Xa and selectivity against thrombin
10. Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa
11. Aminoisoquinolines: Design and synthesis of an orally active benzamidine isostere for the inhibition of factor Xa
12. Thrombin inhibitor design
13. Protease inhibitors: Current status and future prospects
14. Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitor
15. Pharmacology of benzamidine-type thrombin inhibitors
16. Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position
17. Sulfonamidopyrrolidinone factor Xa inhibitors: Potency and selectivity enhancements via P-1 and P-4 optimization
18. Processing of X-ray diffraction data collected in oscillation mode
19. RPR120844, a novel specific inhibitor of coagulation factor Xa inhibits venous thrombosis in the rabbit