1f5k

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[[Image:1f5k.jpg|left|200px]]
[[Image:1f5k.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1f5k |SIZE=350|CAPTION= <scene name='initialview01'>1f5k</scene>, resolution 1.8&Aring;
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The line below this paragraph, containing "STRUCTURE_1f5k", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=BAM:BENZAMIDINE'>BAM</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1f5k| PDB=1f5k | SCENE= }}
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|RELATEDENTRY=[[1ejn|1EJN]], [[1f5l|1F5L]], [[1f92|1F92]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1f5k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1f5k OCA], [http://www.ebi.ac.uk/pdbsum/1f5k PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1f5k RCSB]</span>
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}}
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'''UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-BENZAMIDINE COMPLEX'''
'''UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-BENZAMIDINE COMPLEX'''
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[[Category: Sturzebecher, J.]]
[[Category: Sturzebecher, J.]]
[[Category: Zeslawska, E.]]
[[Category: Zeslawska, E.]]
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[[Category: human]]
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[[Category: Human]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: serine protease]]
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[[Category: Serine protease]]
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[[Category: urokinase]]
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[[Category: Urokinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 15:55:37 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:16:17 2008''
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Revision as of 12:55, 2 May 2008

Image:1f5k.jpg

Template:STRUCTURE 1f5k

UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-BENZAMIDINE COMPLEX


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.

About this Structure

1F5K is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design., Zeslawska E, Schweinitz A, Karcher A, Sondermann P, Sperl S, Sturzebecher J, Jacob U, J Mol Biol. 2000 Aug 11;301(2):465-75. PMID:10926521 Page seeded by OCA on Fri May 2 15:55:37 2008

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