1u6q: Difference between revisions
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|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=745:TRANS-6-(2-PHENYLCYCLOPROPYL)-NAPHTHALENE-2-CARBOXAMIDINE'>745</scene> | |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] | |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> | ||
|GENE= PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
|DOMAIN= | |||
|RELATEDENTRY=[[1owd|1OWD]], [[1owe|1OWE]], [[1owh|1OWH]], [[1owi|1OWI]], [[1owj|1OWJ]], [[1sqa|1SQA]] | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1u6q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1u6q OCA], [http://www.ebi.ac.uk/pdbsum/1u6q PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1u6q RCSB]</span> | |||
}} | }} | ||
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[[Category: Sauer, D R.]] | [[Category: Sauer, D R.]] | ||
[[Category: Wendt, M D.]] | [[Category: Wendt, M D.]] | ||
[[Category: hydrolase]] | [[Category: hydrolase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:06:07 2008'' | ||
Revision as of 21:06, 30 March 2008
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| 1u6q, resolution 2.02Å | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Ligands: | 745 | ||||||||||||
| Gene: | PLAU (Homo sapiens) | ||||||||||||
| Activity: | U-plasminogen activator, with EC number 3.4.21.73 | ||||||||||||
| Related: | 1OWD, 1OWE, 1OWH, 1OWI, 1OWJ, 1SQA
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
Substituted 2-Naphthamadine inhibitors of Urokinase
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
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