6e5l: Difference between revisions

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OCA

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-'''Unreleased structure'''
-The entry 6e5l is ON HOLD  until Paper Publication
+==Crystal structure of human cellular retinol binding protein 1 in complex with abnormal-cannabidiol (abn-CBD)==
+<StructureSection load='6e5l' size='340' side='right'caption='[[6e5l]], [[Resolution|resolution]] 1.17&Aring;' scene=''>
+== Structural highlights ==
+<table><tr><td colspan='2'>[[6e5l]] is a 1 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=6E5L OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6E5L 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]] 1.17&#8491;</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=HVD:(1R,2R)-5-methyl-6-pentyl-2-(prop-1-en-2-yl)-1,2,3,4-tetrahydro[1,1-biphenyl]-2,4-diol'>HVD</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=6e5l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e5l OCA], [https://pdbe.org/6e5l PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6e5l RCSB], [https://www.ebi.ac.uk/pdbsum/6e5l PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6e5l ProSAT]</span></td></tr>
+</table>
+== Function ==
+[https://www.uniprot.org/uniprot/RET1_HUMAN RET1_HUMAN] Intracellular transport of retinol.
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+Cellular retinol-binding proteins (CRBPs) facilitate the uptake and intracellular transport of vitamin A. They integrate retinoid metabolism, playing an important role in regulating the synthesis of bioactive vitamin A metabolites. Thus, CRBPs constitute potential pharmacological targets to modulate cellular retinoid status that in turn may have applications in the treatment of certain immunological, metabolic, and ocular disorders. Here we identify abnormal cannabidiol (abn-CBD) as a nonretinoid inhibitor of cellular retinol-binding protein 1 (CRBP1). X-ray crystal structures of CRBP1 in complex with abn-CBD and its derivatives revealed a distinctive mode of protein-ligand interaction and provided a molecular basis for the high affinity and selectivity of this compound. We demonstrated that abn-CBD modulates the flux of retinoids via the retinoid cycle in vivo. Furthermore, the biological activity of abn-CBD was evidenced by its ability to protect against light-induced retinal damage in Balb/cJ mice. Altogether, our findings indicate that targeting selected CRBPs with a small-molecule inhibitor can potentially lead to the development of new therapeutic agents to counteract diseases with etiologies involving imbalance in retinoid metabolism or signaling.
-Authors:
+Abnormal Cannabidiol Modulates Vitamin A Metabolism by Acting as a Competitive Inhibitor of CRBP1.,Silvaroli JA, Widjaja-Adhi MAK, Trischman T, Chelstowska S, Horwitz S, Banerjee S, Kiser PD, Blaner WS, Golczak M ACS Chem Biol. 2019 Mar 15;14(3):434-448. doi: 10.1021/acschembio.8b01070. Epub, 2019 Feb 18. PMID:30721022<ref>PMID:30721022</ref>
-Description:
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-[[Category: Unreleased Structures]]
+</div>
+<div class="pdbe-citations 6e5l" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[Retinol-binding protein 3D structures|Retinol-binding protein 3D structures]]
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Homo sapiens]]
+[[Category: Large Structures]]
+[[Category: Banerjee S]]
+[[Category: Golczak M]]
+[[Category: Kiser PD]]
+[[Category: Silvaroli JA]]