4yvp: Difference between revisions
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''' | ==Crystal Structure of AKR1C1 complexed with glibenclamide== | ||
<StructureSection load='4yvp' size='340' side='right' caption='[[4yvp]], [[Resolution|resolution]] 2.60Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[4yvp]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4YVP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YVP FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GBM:5-CHLORO-N-(2-{4-[(CYCLOHEXYLCARBAMOYL)SULFAMOYL]PHENYL}ETHYL)-2-METHOXYBENZAMIDE'>GBM</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4yvv|4yvv]], [[4yvx|4yvx]]</td></tr> | |||
<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=4yvp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yvp OCA], [http://pdbe.org/4yvp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yvp RCSB], [http://www.ebi.ac.uk/pdbsum/4yvp PDBsum]</span></td></tr> | |||
</table> | |||
== Function == | |||
[[http://www.uniprot.org/uniprot/AK1C1_HUMAN AK1C1_HUMAN]] Converts progesterone to its inactive form, 20-alpha-dihydroxyprogesterone (20-alpha-OHP). In the liver and intestine, may have a role in the transport of bile. May have a role in monitoring the intrahepatic bile acid concentration. Has a low bile-binding ability. May play a role in myelin formation.<ref>PMID:11013348</ref> <ref>PMID:8573067</ref> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
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. | |||
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> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 4yvp" style="background-color:#fffaf0;"></div> | |||
[[Category: | == References == | ||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Hu, X]] | |||
[[Category: Zhang, H]] | [[Category: Zhang, H]] | ||
[[Category: Zhao, Y]] | |||
[[Category: Zheng, X]] | [[Category: Zheng, X]] | ||
[[Category: | [[Category: Akr1c1 inhibitor]] | ||
[[Category: | [[Category: Oxidoreductase-oxidoreductase inhibitor complex]] | ||
Revision as of 07:32, 1 December 2015
Crystal Structure of AKR1C1 complexed with glibenclamideCrystal Structure of AKR1C1 complexed with glibenclamide
Structural highlights
Function[AK1C1_HUMAN] Converts progesterone to its inactive form, 20-alpha-dihydroxyprogesterone (20-alpha-OHP). In the liver and intestine, may have a role in the transport of bile. May have a role in monitoring the intrahepatic bile acid concentration. Has a low bile-binding ability. May play a role in myelin formation.[1] [2] Publication Abstract from PubMedRecent 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. 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[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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