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4zfc

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==Crystal structure of AKR1C3 complexed with glicazide==
==Crystal structure of AKR1C3 complexed with glicazide==
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<StructureSection load='4zfc' size='340' side='right' caption='[[4zfc]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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<StructureSection load='4zfc' size='340' side='right'caption='[[4zfc]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4zfc]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZFC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZFC FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4zfc]] is a 2 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=4ZFC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ZFC FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GCZ:N-[(3AR,6AS)-HEXAHYDROCYCLOPENTA[C]PYRROL-2(1H)-YLCARBAMOYL]-4-METHYLBENZENESULFONAMIDE'>GCZ</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene></td></tr>
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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&#8491;</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4zfc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zfc OCA], [http://pdbe.org/4zfc PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4zfc RCSB], [http://www.ebi.ac.uk/pdbsum/4zfc PDBsum]</span></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=GCZ:N-[(3AR,6AS)-HEXAHYDROCYCLOPENTA[C]PYRROL-2(1H)-YLCARBAMOYL]-4-METHYLBENZENESULFONAMIDE'>GCZ</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene></td></tr>
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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=4zfc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zfc OCA], [https://pdbe.org/4zfc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4zfc RCSB], [https://www.ebi.ac.uk/pdbsum/4zfc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4zfc ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/AK1C3_HUMAN AK1C3_HUMAN]] Catalyzes the conversion of aldehydes and ketones to alcohols. Catalyzes the reduction of prostaglandin (PG) D2, PGH2 and phenanthrenequinone (PQ) and the oxidation of 9-alpha,11-beta-PGF2 to PGD2. Functions as a bi-directional 3-alpha-, 17-beta- and 20-alpha HSD. Can interconvert active androgens, estrogens and progestins with their cognate inactive metabolites. Preferentially transforms androstenedione (4-dione) to testosterone.
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[https://www.uniprot.org/uniprot/AK1C3_HUMAN AK1C3_HUMAN] Catalyzes the conversion of aldehydes and ketones to alcohols. Catalyzes the reduction of prostaglandin (PG) D2, PGH2 and phenanthrenequinone (PQ) and the oxidation of 9-alpha,11-beta-PGF2 to PGD2. Functions as a bi-directional 3-alpha-, 17-beta- and 20-alpha HSD. Can interconvert active androgens, estrogens and progestins with their cognate inactive metabolites. Preferentially transforms androstenedione (4-dione) to testosterone.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Recent epidemiological studies show conflicting data for the first-line anti-diabetic sulphonylureas drugs in treating cancer progression in type II diabetes patients. How sulphonylureas promote or diminish tumor growth is not fully understood. Here, we report that seven sulphonylureas exhibit different in vitro inhibition towards AKR1Cs (AKR1C1, AKR1C2, AKR1C3), which are critical steroid hormone metabolism enzymes that are related to prostate cancer, breast cancer and endometrial diseases. Interactions of the sulphonylureas and AKR1Cs were analyzed by X-ray crystallography.
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In vitro inhibition of AKR1Cs by sulphonylureas and the structural basis.,Zhao Y, Zheng X, Zhang H, Zhai J, Zhang L, Li C, Zeng K, Chen Y, Li Q, Hu X Chem Biol Interact. 2015 Oct 5;240:310-5. doi: 10.1016/j.cbi.2015.09.006. Epub, 2015 Sep 8. PMID:26362498<ref>PMID:26362498</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4zfc" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Hu, X]]
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[[Category: Homo sapiens]]
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[[Category: Zhao, Y]]
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[[Category: Large Structures]]
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[[Category: Zhrng, X]]
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[[Category: Hu X]]
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[[Category: Akr1c3 inhibitor]]
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[[Category: Zhao Y]]
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[[Category: Oxidoreductase-oxidoreductase inhibitor complex]]
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[[Category: Zhrng X]]

Current revision

Crystal structure of AKR1C3 complexed with glicazide

PDB ID 4zfc

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