1u6q

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[[Image:1u6q.jpg|left|200px]]
 
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==Substituted 2-Naphthamadine inhibitors of Urokinase==
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The line below this paragraph, containing "STRUCTURE_1u6q", creates the "Structure Box" on the page.
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<StructureSection load='1u6q' size='340' side='right'caption='[[1u6q]], [[Resolution|resolution]] 2.02&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[1u6q]] is a 1 chain structure with sequence from [https://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]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1U6Q FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.02&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=745:TRANS-6-(2-PHENYLCYCLOPROPYL)-NAPHTHALENE-2-CARBOXAMIDINE'>745</scene></td></tr>
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{{STRUCTURE_1u6q| PDB=1u6q | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1u6q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1u6q OCA], [https://pdbe.org/1u6q PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1u6q RCSB], [https://www.ebi.ac.uk/pdbsum/1u6q PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1u6q ProSAT]</span></td></tr>
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</table>
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'''Substituted 2-Naphthamadine inhibitors of Urokinase'''
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== Disease ==
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[https://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[https://omim.org/entry/601709 601709]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>
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== Function ==
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==Overview==
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[https://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/u6/1u6q_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1u6q ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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.
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.
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==Disease==
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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<ref>PMID:15582418</ref>
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Known disease associated with this structure: Alzheimer disease, late-onset, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=191840 191840]]
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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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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].
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</div>
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<div class="pdbe-citations 1u6q" style="background-color:#fffaf0;"></div>
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==Reference==
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==See Also==
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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]
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*[[Urokinase 3D Structures|Urokinase 3D Structures]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Single protein]]
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[[Category: Large Structures]]
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[[Category: U-plasminogen activator]]
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[[Category: Bruncko M]]
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[[Category: Bruncko, M.]]
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[[Category: Dalton CR]]
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[[Category: Dalton, C R.]]
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[[Category: Geyer A]]
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[[Category: Geyer, A.]]
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[[Category: Giranda VL]]
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[[Category: Giranda, V L.]]
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[[Category: Kaminski MK]]
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[[Category: Kaminski, M K.]]
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[[Category: McClellan W]]
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[[Category: McClellan, W.]]
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[[Category: Nienaber VL]]
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[[Category: Nienaber, V L.]]
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[[Category: Rockway TR]]
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[[Category: Rockway, T R.]]
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[[Category: Sauer DR]]
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[[Category: Sauer, D R.]]
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[[Category: Wendt MD]]
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[[Category: Wendt, M D.]]
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[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:49:39 2008''
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Current revision

Substituted 2-Naphthamadine inhibitors of Urokinase

PDB ID 1u6q

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