1nt1: Difference between revisions
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==Overview== | ==Overview== | ||
A series of potent and selective proline- and pyrazinone-based macrocyclic | A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. Detailed SAR studies led to the incorporation of specific functional groups in the tether that enhanced functional activity against thrombin and provided exquisite selectivity against trypsin and tPA. X-ray crystallography and molecular modeling studies revealed the inhibitor-enzyme interactions responsible for this selectivity. | ||
==Disease== | ==Disease== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Thrombin]] | [[Category: Thrombin]] | ||
[[Category: Barrow, J | [[Category: Barrow, J C.]] | ||
[[Category: Krueger, J | [[Category: Krueger, J A.]] | ||
[[Category: Kuo, L | [[Category: Kuo, L C.]] | ||
[[Category: Lewis, S | [[Category: Lewis, S D.]] | ||
[[Category: Lucas, B | [[Category: Lucas, B J.]] | ||
[[Category: McMasters, D | [[Category: McMasters, D R.]] | ||
[[Category: Nantermet, P | [[Category: Nantermet, P G.]] | ||
[[Category: Newton, C | [[Category: Newton, C L.]] | ||
[[Category: Pellicore, J | [[Category: Pellicore, J M.]] | ||
[[Category: Selnick, H | [[Category: Selnick, H G.]] | ||
[[Category: Vacca, J | [[Category: Vacca, J P.]] | ||
[[Category: Yan, Y.]] | [[Category: Yan, Y.]] | ||
[[Category: Young, M.]] | [[Category: Young, M.]] | ||
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[[Category: thrombin inhibitor complex]] | [[Category: thrombin inhibitor complex]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:09:39 2008'' | ||
