1sqt: Difference between revisions

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[[Image:1sqt.jpg|left|200px]]
[[Image:1sqt.jpg|left|200px]]


{{Structure
<!--
|PDB= 1sqt |SIZE=350|CAPTION= <scene name='initialview01'>1sqt</scene>, resolution 1.90&Aring;
The line below this paragraph, containing "STRUCTURE_1sqt", creates the "Structure Box" on the page.
|SITE=
You may change the PDB parameter (which sets the PDB file loaded into the applet)  
|LIGAND= <scene name='pdbligand=UI3:7-METHOXY-8-[1-(METHYLSULFONYL)-1H-PYRAZOL-4-YL]NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI3</scene>
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
|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>
or leave the SCENE parameter empty for the default display.
|GENE= PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
-->
|DOMAIN=
{{STRUCTURE_1sqt|  PDB=1sqt |  SCENE= }}  
|RELATEDENTRY=[[1owd|1OWD]], [[1owe|1OWE]], [[1owh|1OWH]], [[1owi|1OWI]], [[1owj|1OWJ]], [[1owk|1OWK]], [[1sqa|1SQA]], [[1sqo|1SQO]]
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1sqt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqt OCA], [http://www.ebi.ac.uk/pdbsum/1sqt PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1sqt RCSB]</span>
}}


'''Substituted 2-Naphthamidine Inhibitors of Urokinase'''
'''Substituted 2-Naphthamidine Inhibitors of Urokinase'''
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[[Category: Wendt, M D.]]
[[Category: Wendt, M D.]]
[[Category: Zhang, X.]]
[[Category: Zhang, X.]]
[[Category: egf-like domain]]
[[Category: Egf-like domain]]
[[Category: glycoprotein]]
[[Category: Glycoprotein]]
[[Category: hydrolase]]
[[Category: Hydrolase]]
[[Category: kringle]]
[[Category: Kringle]]
[[Category: plasminogen activation]]
[[Category: Plasminogen activation]]
[[Category: serine protease]]
[[Category: Serine protease]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 09:02:17 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:45:48 2008''

Revision as of 09:02, 3 May 2008

File:1sqt.jpg

Template:STRUCTURE 1sqt

Substituted 2-Naphthamidine Inhibitors of Urokinase


OverviewOverview

Several 8-substituted 2-naphthamidine-based inhibitors of the serine protease urokinase plasminogen activator (uPA) are described. Direct attachment of five-membered saturated or unsaturated rings improved inhibitor performance; substitution with sulfones further improved binding profiles. Combination of these substituents or of previously described NH-linked heteroaromatic rings with 6-phenyl amide substituents provided further enhancements to potency and selectivity.

DiseaseDisease

Known disease associated with this structure: Alzheimer disease, late-onset, susceptibility to OMIM:[191840]

About this StructureAbout this Structure

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

ReferenceReference

Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors., Wendt MD, Geyer A, McClellan WJ, Rockway TW, Weitzberg M, Zhao X, Mantei R, Stewart K, Nienaber V, Klinghofer V, Giranda VL, Bioorg Med Chem Lett. 2004 Jun 21;14(12):3063-8. PMID:15149645 Page seeded by OCA on Sat May 3 09:02:17 2008

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OCA
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