View source for 5tiy


==Schistosoma haematobium (Blood Fluke) Sulfotransferase/S-oxamniquine Complex==
<StructureSection load='5tiy' size='340' side='right'caption='[[5tiy]], [[Resolution|resolution]] 1.76&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5tiy]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Schistosoma_haematobium Schistosoma haematobium]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TIY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5TIY FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.76&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A3P:ADENOSINE-3-5-DIPHOSPHATE'>A3P</scene>, <scene name='pdbligand=OAQ:{(2S)-7-NITRO-2-[(PROPAN-2-YLAMINO)METHYL]-1,2,3,4-TETRAHYDROQUINOLIN-6-YL}METHANOL'>OAQ</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=5tiy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tiy OCA], [https://pdbe.org/5tiy PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5tiy RCSB], [https://www.ebi.ac.uk/pdbsum/5tiy PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5tiy ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/A0A094ZWQ2_SCHHA A0A094ZWQ2_SCHHA] 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The antischistosomal prodrug oxamniquine is activated by a sulfotransferase (SULT) in the parasitic flatworm Schistosoma mansoni. Of the three main human schistosome species, only S. mansoni is sensitive to oxamniquine therapy despite the presence of SULT orthologs in Schistosoma hematobium and Schistosoma japonicum The reason for this species-specific drug action has remained a mystery for decades. Here we present the crystal structures of S. hematobium and S. japonicum SULTs, including S. hematobium SULT in complex with oxamniquine. We also examined the activity of the three enzymes in vitro; surprisingly, all three are active toward oxamniquine, yet we observed differences in catalytic efficiency that implicate kinetics as the determinant for species-specific toxicity. These results provide guidance for designing oxamniquine derivatives to treat infection caused by all species of schistosome to combat emerging resistance to current therapy.

Structural and enzymatic insights into species-specific resistance to schistosome parasite drug therapy.,Taylor AB, Roberts KM, Cao X, Clark NE, Holloway SP, Donati E, Polcaro CM, Pica-Mattoccia L, Tarpley RS, McHardy SF, Cioli D, LoVerde PT, Fitzpatrick PF, Hart PJ J Biol Chem. 2017 Jul 7;292(27):11154-11164. doi: 10.1074/jbc.M116.766527. Epub, 2017 May 23. PMID:28536265<ref>PMID:28536265</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 5tiy" style="background-color:#fffaf0;"></div>

==See Also==
*[[Sulfotransferase 3D structures|Sulfotransferase 3D structures]]
== References ==
<references/>
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</StructureSection>
[[Category: Large Structures]]
[[Category: Schistosoma haematobium]]
[[Category: Hart PJ]]
[[Category: Taylor AB]]