1w7g: Difference between revisions
From Proteopedia
Jump to navigationJump to search
No edit summary |
No edit summary |
||
| Line 5: | Line 5: | ||
==Overview== | ==Overview== | ||
Piperazinyl-amide derivatives of, N-alpha-(3-trifluoromethyl-benzenesulfonyl)-L-arginine (1) were, synthesized as graftable thrombin inhibitors. The possible disturbance of, biological activity due to a variable spacer-arm fixed on the N-4, piperazinyl position was evaluated in vitro, against human alpha-thrombin, and in blood coagulation assay. Molecular modelling (in silico analysis), and X-ray diffraction studies of thrombin-inhibitor complexes were also, performed. The fixation of bioactive molecules on poly(butylene, terephthalate) (PBT) and poly(ethylene terephthalate) (PET) membranes was, performed by wet chemistry treatment and evaluated by XPS analysis., Surface grafting of inhibitor 1d improved the membrane hemocompatibility, by reducing blood clot formation on the modified . | Piperazinyl-amide derivatives of, N-alpha-(3-trifluoromethyl-benzenesulfonyl)-L-arginine (1) were, synthesized as graftable thrombin inhibitors. The possible disturbance of, biological activity due to a variable spacer-arm fixed on the N-4, piperazinyl position was evaluated in vitro, against human alpha-thrombin, and in blood coagulation assay. Molecular modelling (in silico analysis), and X-ray diffraction studies of thrombin-inhibitor complexes were also, performed. The fixation of bioactive molecules on poly(butylene, terephthalate) (PBT) and poly(ethylene terephthalate) (PET) membranes was, performed by wet chemistry treatment and evaluated by XPS analysis., Surface grafting of inhibitor 1d improved the membrane hemocompatibility, by reducing blood clot formation on the modified surface. | ||
==About this Structure== | ==About this Structure== | ||
1W7G is a | 1W7G is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MIU as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1W7G OCA]. | ||
==Reference== | ==Reference== | ||
| Line 25: | Line 25: | ||
[[Category: thrombin]] | [[Category: thrombin]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 15:23:37 2007'' | ||
