1fv9

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[[Image:1fv9.gif|left|200px]]
 
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{{Structure
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==Crystal structure of human microurokinase in complex with 2-amino-5-hydroxy-benzimidazole==
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|PDB= 1fv9 |SIZE=350|CAPTION= <scene name='initialview01'>1fv9</scene>, resolution 3.00&Aring;
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<StructureSection load='1fv9' size='340' side='right'caption='[[1fv9]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <scene name='pdbligand=172:2-AMINO-5-HYDROXY-BENZIMIDAZOLE'>172</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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<table><tr><td colspan='2'>[[1fv9]] 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=1FV9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1FV9 FirstGlance]. <br>
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|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>
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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]] 3&#8491;</td></tr>
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|GENE=
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=172:2-AMINO-5-HYDROXY-BENZIMIDAZOLE'>172</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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|DOMAIN=
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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=1fv9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1fv9 OCA], [https://pdbe.org/1fv9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1fv9 RCSB], [https://www.ebi.ac.uk/pdbsum/1fv9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1fv9 ProSAT]</span></td></tr>
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|RELATEDENTRY=
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</table>
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1fv9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1fv9 OCA], [http://www.ebi.ac.uk/pdbsum/1fv9 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1fv9 RCSB]</span>
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== Disease ==
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}}
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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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[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/fv/1fv9_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.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=1fv9 ConSurf].
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<div style="clear:both"></div>
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'''Crystal structure of human microurokinase in complex with 2-amino-5-hydroxy-benzimidazole'''
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==See Also==
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*[[Urokinase 3D Structures|Urokinase 3D Structures]]
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== References ==
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==Overview==
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<references/>
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Using an NMR-based screen, a novel class of urokinase inhibitors were identified that contain a 2-aminobenzimidazole moiety. The inhibitory potency of this family of inhibitors is similar to that of inhibitors containing a guanidine or amidine group. However, unlike previously described guanidino- or amidino-based inhibitors which have pK(a) values greater than 9.0, urokinase inhibitors containing a 2-aminobenzimidazole have pK(a) values of 7.5. Thus, 2-aminobenzimidazoles may have improved pharmacokinetic properties which could increase the bioavailability of inhibitors which contain this moiety. A crystal structure of one of the lead inhibitors, 2-amino-5-hydroxybenzimidazole, complexed with urokinase reveals the electrostatic and hydrophobic interactions that stabilize complex formation and suggests nearby subsites that may be accessed to increase the potency of this new series of urokinase inhibitors.
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__TOC__
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</StructureSection>
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==About this Structure==
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1FV9 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=1FV9 OCA].
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==Reference==
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Identification of novel inhibitors of urokinase via NMR-based screening., Hajduk PJ, Boyd S, Nettesheim D, Nienaber V, Severin J, Smith R, Davidson D, Rockway T, Fesik SW, J Med Chem. 2000 Oct 19;43(21):3862-6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11052791 11052791]
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[[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: Nienaber V]]
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[[Category: Nienaber, V.]]
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[[Category: plasminogen activation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:30:57 2008''
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Current revision

Crystal structure of human microurokinase in complex with 2-amino-5-hydroxy-benzimidazole

PDB ID 1fv9

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