1f5l: Difference between revisions

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==Overview==

Urokinase is a serine protease involved in cancer growth and metastasis., Here we present the first urokinase crystal structure in complex with, reversible inhibitors at 2.1 and 2.6 A resolution. These inhibitor complex, structures have been obtained from crystals of engineered urokinase type, plasminogen activator designed to obtain a crystal form open for inhibitor, soaking. The mutant C122S loses its flexible A-chain upon activation, cleavage and crystallizes in the presence of benzamidine, which was later, displaced by the desired inhibitor. This new soakable crystal form turned, out to be of great value in the process of structure-based drug design., The evaluated binding mode of amiloride, and UKI-1D revealed a new subsite, of the primary specificity pocket of urokinase that will be employed in, the future ligand optimisation process.

Urokinase is a serine protease involved in cancer growth and metastasis. Here we present the first urokinase crystal structure in complex with reversible inhibitors at 2.1 and 2.6 A resolution. These inhibitor complex structures have been obtained from crystals of engineered urokinase type plasminogen activator designed to obtain a crystal form open for inhibitor soaking. The mutant C122S loses its flexible A-chain upon activation cleavage and crystallizes in the presence of benzamidine, which was later displaced by the desired inhibitor. This new soakable crystal form turned out to be of great value in the process of structure-based drug design. The evaluated binding mode of amiloride, and UKI-1D revealed a new subsite of the primary specificity pocket of urokinase that will be employed in the future ligand optimisation process.

==Disease==

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[[Category: urokinase]]

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@@ Line 4: / Line 4: @@
 ==Overview==
-Urokinase is a serine protease involved in cancer growth and metastasis., Here we present the first urokinase crystal structure in complex with, reversible inhibitors at 2.1 and 2.6 A resolution. These inhibitor complex, structures have been obtained from crystals of engineered urokinase type, plasminogen activator designed to obtain a crystal form open for inhibitor, soaking. The mutant C122S loses its flexible A-chain upon activation, cleavage and crystallizes in the presence of benzamidine, which was later, displaced by the desired inhibitor. This new soakable crystal form turned, out to be of great value in the process of structure-based drug design., The evaluated binding mode of amiloride, and UKI-1D revealed a new subsite, of the primary specificity pocket of urokinase that will be employed in, the future ligand optimisation process.
+Urokinase is a serine protease involved in cancer growth and metastasis. Here we present the first urokinase crystal structure in complex with reversible inhibitors at 2.1 and 2.6 A resolution. These inhibitor complex structures have been obtained from crystals of engineered urokinase type plasminogen activator designed to obtain a crystal form open for inhibitor soaking. The mutant C122S loses its flexible A-chain upon activation cleavage and crystallizes in the presence of benzamidine, which was later displaced by the desired inhibitor. This new soakable crystal form turned out to be of great value in the process of structure-based drug design. The evaluated binding mode of amiloride, and UKI-1D revealed a new subsite of the primary specificity pocket of urokinase that will be employed in the future ligand optimisation process.
 ==Disease==
@@ Line 31: / Line 31: @@
 [[Category: urokinase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 15:46:00 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:35:06 2008''