1f5k

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[[Image:1f5k.jpg|left|200px]]
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{{Seed}}
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[[Image:1f5k.png|left|200px]]
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{{STRUCTURE_1f5k| PDB=1f5k | SCENE= }}
{{STRUCTURE_1f5k| PDB=1f5k | SCENE= }}
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'''UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-BENZAMIDINE COMPLEX'''
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===UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-BENZAMIDINE COMPLEX===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 10926521 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10926521}}
==About this Structure==
==About this Structure==
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[[Category: Serine protease]]
[[Category: Serine protease]]
[[Category: Urokinase]]
[[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 Tue Jul 1 02:43:53 2008''

Revision as of 23:43, 30 June 2008

Image:1f5k.png

Template:STRUCTURE 1f5k

UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-BENZAMIDINE COMPLEX

Template:ABSTRACT PUBMED 10926521

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

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