6zja: Difference between revisions
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==Helicobacter pylori urease with inhibitor bound in the active site== | |||
<StructureSection load='6zja' size='340' side='right'caption='[[6zja]], [[Resolution|resolution]] 2.00Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[6zja]] is a 24 chain structure with sequence from [https://en.wikipedia.org/wiki/Helicobacter_pylori Helicobacter pylori]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6ZJA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZJA FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 2Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DJM:2-[1-(3,5-dimethylphenyl)imidazol-2-yl]sulfanyl-~{N}-oxidanyl-ethanamide'>DJM</scene>, <scene name='pdbligand=KCX:LYSINE+NZ-CARBOXYLIC+ACID'>KCX</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6zja FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zja OCA], [https://pdbe.org/6zja PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zja RCSB], [https://www.ebi.ac.uk/pdbsum/6zja PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zja ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/URE23_HELPY URE23_HELPY] Ammonia produced by ureolysis increases the gastric pH thereby providing an environment permissive for colonization of the stomach.<ref>PMID:8039935</ref> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Infection of the human stomach by Helicobacter pylori remains a worldwide problem and greatly contributes to peptic ulcer disease and gastric cancer. Without active intervention approximately 50% of the world population will continue to be infected with this gastric pathogen. Current eradication, called triple therapy, entails a proton-pump inhibitor and two broadband antibiotics, however resistance to either clarithromycin or metronidazole is greater than 25% and rising. Therefore, there is an urgent need for a targeted, high-specificity eradication drug. Gastric infection by H. pylori depends on the expression of a nickel-dependent urease in the cytoplasm of the bacteria. Here, we report the 2.0 A resolution structure of the 1.1 MDa urease in complex with an inhibitor by cryo-electron microscopy and compare it to a beta-mercaptoethanol-inhibited structure at 2.5 A resolution. The structural information is of sufficient detail to aid in the development of inhibitors with high specificity and affinity. | |||
Cryo-EM structure of Helicobacter pylori urease with an inhibitor in the active site at 2.0 A resolution.,Cunha ES, Chen X, Sanz-Gaitero M, Mills DJ, Luecke H Nat Commun. 2021 Jan 11;12(1):230. doi: 10.1038/s41467-020-20485-6. PMID:33431861<ref>PMID:33431861</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
<div class="pdbe-citations 6zja" style="background-color:#fffaf0;"></div> | |||
==See Also== | |||
*[[Urease 3D structures|Urease 3D structures]] | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Helicobacter pylori]] | |||
[[Category: Large Structures]] | |||
[[Category: Cunha E]] | |||
[[Category: Luecke H]] | |||
