1u6q
From Proteopedia
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| - | [[Image:1u6q.jpg|left|200px]] | + | [[Image:1u6q.jpg|left|200px]] |
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| - | '''Substituted 2-Naphthamadine inhibitors of Urokinase''' | + | {{Structure |
| + | |PDB= 1u6q |SIZE=350|CAPTION= <scene name='initialview01'>1u6q</scene>, resolution 2.02Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=745:TRANS-6-(2-PHENYLCYCLOPROPYL)-NAPHTHALENE-2-CARBOXAMIDINE'>745</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''Substituted 2-Naphthamadine inhibitors of Urokinase''' | ||
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==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1U6Q is a [ | + | 1U6Q is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1U6Q OCA]. |
==Reference== | ==Reference== | ||
| - | Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties., Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL, Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8. PMID:[http:// | + | Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties., Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL, Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15582418 15582418] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:28:08 2008'' |
Revision as of 12:28, 20 March 2008
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| , resolution 2.02Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | PLAU (Homo sapiens) | ||||||
| Activity: | U-plasminogen activator, with EC number 3.4.21.73 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Substituted 2-Naphthamadine inhibitors of Urokinase
Contents |
Overview
A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.
Disease
Known disease associated with this structure: Alzheimer disease, late-onset, susceptibility to OMIM:[191840]
About this Structure
1U6Q is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties., Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL, Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8. PMID:15582418
Page seeded by OCA on Thu Mar 20 14:28:08 2008
