6jno: Difference between revisions

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-'''Unreleased structure'''
-The entry 6jno is ON HOLD  until Paper Publication
+==RXRa structure complexed with CU-6PMN==
+<StructureSection load='6jno' size='340' side='right'caption='[[6jno]], [[Resolution|resolution]] 2.65&Aring;' scene=''>
+== Structural highlights ==
+<table><tr><td colspan='2'>[[6jno]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5gym 5gym]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6JNO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6JNO 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]] 2.65&#8491;</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=WY5:7-oxidanyl-2-oxidanylidene-6-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)chromene-3-carboxylic+acid'>WY5</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=6jno FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6jno OCA], [https://pdbe.org/6jno PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6jno RCSB], [https://www.ebi.ac.uk/pdbsum/6jno PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6jno ProSAT]</span></td></tr>
+</table>
+== Function ==
+[https://www.uniprot.org/uniprot/RXRA_HUMAN RXRA_HUMAN] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid. RXRA serves as a common heterodimeric partner for a number of nuclear receptors. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes.<ref>PMID:10195690</ref> <ref>PMID:11162439</ref> <ref>PMID:11915042</ref> <ref>PMID:20215566</ref>
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+Ligands for retinoid X receptors (RXRs), "rexinoids", are attracting interest as candidates for therapy of type 2 diabetes and Alzheimer's and Parkinson's diseases. However, current screening methods for rexinoids are slow and require special apparatus or facilities. Here, we created 7-hydroxy-2-oxo-6-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-2H-ch romene-3-carboxylic acid (10, CU-6PMN) as a new fluorescent RXR agonist and developed a screening system of rexinoids using 10. Compound 10 was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay using 10 enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such as filtration.
-Authors: Kawasaki, M., Nakano, S., Motoyama, T., Yamada, S., Watanabe, M., Takamura, Y., Fujihara, M., Tokiwa, H., Kakuta, H., Ito, S.
+Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for Retinoid X Receptor Ligand Screening.,Yamada S, Kawasaki M, Fujihara M, Watanabe M, Takamura Y, Takioku M, Nishioka H, Takeuchi Y, Makishima M, Motoyama T, Ito S, Tokiwa H, Nakano S, Kakuta H J Med Chem. 2019 Oct 10;62(19):8809-8818. doi: 10.1021/acs.jmedchem.9b00995. Epub, 2019 Sep 18. PMID:31483660<ref>PMID:31483660</ref>
-Description: RXRa structure complexed with CU-6PMN
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-[[Category: Unreleased Structures]]
+</div>
-[[Category: Yamada, S]]
+<div class="pdbe-citations 6jno" style="background-color:#fffaf0;"></div>
-[[Category: Motoyama, T]]
-[[Category: Watanabe, M]]
+==See Also==
-[[Category: Ito, S]]
+*[[Retinoid X receptor 3D structures|Retinoid X receptor 3D structures]]
-[[Category: Nakano, S]]
+== References ==
-[[Category: Takamura, Y]]
+<references/>
-[[Category: Tokiwa, H]]
+__TOC__
-[[Category: Fujihara, M]]
+</StructureSection>
-[[Category: Kawasaki, M]]
+[[Category: Homo sapiens]]
-[[Category: Kakuta, H]]
+[[Category: Large Structures]]
+[[Category: Fujihara M]]
+[[Category: Ito S]]
+[[Category: Kakuta H]]
+[[Category: Kawasaki M]]
+[[Category: Motoyama T]]
+[[Category: Nakano S]]
+[[Category: Takamura Y]]
+[[Category: Tokiwa H]]
+[[Category: Watanabe M]]
+[[Category: Yamada S]]