|
|
| Line 1: |
Line 1: |
| [[Image:1zom.gif|left|200px]] | | {{Seed}} |
| | [[Image:1zom.png|left|200px]] |
|
| |
|
| <!-- | | <!-- |
| Line 9: |
Line 10: |
| {{STRUCTURE_1zom| PDB=1zom | SCENE= }} | | {{STRUCTURE_1zom| PDB=1zom | SCENE= }} |
|
| |
|
| '''Crystal Structure of the Catalytic Domain of Coagulation Factor XI in complex with a peptidomimetic Inhibitor'''
| | ===Crystal Structure of the Catalytic Domain of Coagulation Factor XI in complex with a peptidomimetic Inhibitor=== |
|
| |
|
|
| |
|
| ==Overview==
| | <!-- |
| Human coagulation factor XIa (FXIa), a serine protease activated by site-specific cleavage of factor XI by thrombin, FXIIa, or autoactivation, is a critical enzyme in the amplification phase of the coagulation cascade. To investigate the potential of FXIa inhibitors as safe anticoagulants, a series of potent, selective peptidomimetic inhibitors of FXIa were designed and synthesized. Some of these inhibitors showed low nanomolar FXIa inhibitory activity with >1000-fold FXa selectivity and >100-fold thrombin selectivity. The X-ray structure of one of these inhibitors, 36, demonstrates its unique binding interactions with FXIa. Compound 32 caused a doubling of the activated partial thromboplastin time in human plasma at 2.4 microM and was efficacious in a rat model of venous thrombosis. These data suggest that factor XIa plays a significant role in venous thrombosis and may be a suitable target for the development of antithrombotic therapy.
| | The line below this paragraph, {{ABSTRACT_PUBMED_17181160}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 17181160 is the PubMed ID number. |
| | --> |
| | {{ABSTRACT_PUBMED_17181160}} |
|
| |
|
| ==Disease== | | ==Disease== |
| Line 38: |
Line 42: |
| [[Category: Fxia]] | | [[Category: Fxia]] |
| [[Category: Inhibitor]] | | [[Category: Inhibitor]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:53:01 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:24:24 2008'' |