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==Helicobacter pylori Xanthine-Guanine-Hypoxanthine Phosphoribosyltransferase== | ==Helicobacter pylori Xanthine-Guanine-Hypoxanthine Phosphoribosyltransferase== | ||
<StructureSection load='7kl6' size='340' side='right'caption='[[7kl6]]' scene=''> | <StructureSection load='7kl6' size='340' side='right'caption='[[7kl6]], [[Resolution|resolution]] 1.97Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7KL6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7KL6 FirstGlance]. <br> | <table><tr><td colspan='2'>[[7kl6]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Atcc_43504 Atcc 43504]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7KL6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7KL6 FirstGlance]. <br> | ||
</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=7kl6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7kl6 OCA], [https://pdbe.org/7kl6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7kl6 RCSB], [https://www.ebi.ac.uk/pdbsum/7kl6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7kl6 ProSAT]</span></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=WG7:(3-{[(4-oxo-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]amino}propyl)phosphonic+acid'>WG7</scene></td></tr> | ||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BXP09_04485, CV723_04510 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=210 ATCC 43504])</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=7kl6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7kl6 OCA], [https://pdbe.org/7kl6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7kl6 RCSB], [https://www.ebi.ac.uk/pdbsum/7kl6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7kl6 ProSAT]</span></td></tr> | |||
</table> | </table> | ||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Helicobacter pylori (Hp) is a human pathogen that lives in the gastric mucosa of approximately 50% of the world's population causing gastritis, peptic ulcers, and gastric cancer. An increase in resistance to current drugs has sparked the search for new Hp drug targets and therapeutics. One target is the disruption of nucleic acid production, which can be achieved by impeding the synthesis of 6-oxopurine nucleoside monophosphates, the precursors of DNA and RNA. These metabolites are synthesized by Hp xanthine-guanine-hypoxanthine phosphoribosyltransferase (XGHPRT). Here, nucleoside phosphonates have been evaluated, which inhibit the activity of this enzyme with Ki values as low as 200 nM. The prodrugs of these compounds arrest the growth of Hp at a concentration of 50 muM in cell-based assays. The kinetic properties of HpXGHPRT have been determined together with its X-ray crystal structure in the absence and presence of 9-[(N-3-phosphonopropyl)-aminomethyl-9-deazahypoxanthine, providing a basis for new antibiotic development. | |||
Helicobacter pylori Xanthine-Guanine-Hypoxanthine Phosphoribosyltransferase-A Putative Target for Drug Discovery against Gastrointestinal Tract Infections.,Keough DT, Wun SJ, Baszczynski O, Eng WS, Spacek P, Panjikar S, Naesens L, Pohl R, Rejman D, Hockova D, Ferrero RL, Guddat LW J Med Chem. 2021 Apr 23. doi: 10.1021/acs.jmedchem.0c02184. PMID:33891818<ref>PMID:33891818</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 7kl6" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Atcc 43504]] | |||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Guddat | [[Category: Guddat, L W]] | ||
[[Category: Keough | [[Category: Keough, D T]] | ||
[[Category: Helicobacter pylori xanthine-guanine-hypoxanthine phosphoribosyltransferase drug discovery nucleoside phosphonate]] | |||
[[Category: Transferase]] | |||