6e5t: Difference between revisions
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<StructureSection load='6e5t' size='340' side='right'caption='[[6e5t]], [[Resolution|resolution]] 1.55Å' scene=''> | <StructureSection load='6e5t' size='340' side='right'caption='[[6e5t]], [[Resolution|resolution]] 1.55Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[6e5t]] is a 1 chain structure with sequence from [ | <table><tr><td colspan='2'>[[6e5t]] 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=6E5T OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6E5T FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=HVJ:(1R,2R)-5,6-dimethyl-2-(prop-1-en-2-yl)-1,2,3,4-tetrahydro[1,1-biphenyl]-2,4-diol'>HVJ</scene> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.55Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=HVJ:(1R,2R)-5,6-dimethyl-2-(prop-1-en-2-yl)-1,2,3,4-tetrahydro[1,1-biphenyl]-2,4-diol'>HVJ</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6e5t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e5t OCA], [https://pdbe.org/6e5t PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6e5t RCSB], [https://www.ebi.ac.uk/pdbsum/6e5t PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6e5t ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
[ | [https://www.uniprot.org/uniprot/RET1_HUMAN RET1_HUMAN] Intracellular transport of retinol. | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</div> | </div> | ||
<div class="pdbe-citations 6e5t" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 6e5t" style="background-color:#fffaf0;"></div> | ||
==See Also== | |||
*[[Retinol-binding protein 3D structures|Retinol-binding protein 3D structures]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Banerjee | [[Category: Banerjee S]] | ||
[[Category: Golczak | [[Category: Golczak M]] | ||
[[Category: Horwitz | [[Category: Horwitz S]] | ||
[[Category: Kiser | [[Category: Kiser PD]] | ||
[[Category: Silvaroli | [[Category: Silvaroli JA]] | ||
Latest revision as of 09:19, 11 October 2023
Crystal structure of human cellular retinol binding protein 1 in complex with abnormal-cannabidiorcin (Abn-CBDO)Crystal structure of human cellular retinol binding protein 1 in complex with abnormal-cannabidiorcin (Abn-CBDO)
Structural highlights
FunctionRET1_HUMAN Intracellular transport of retinol. Publication Abstract from PubMedCellular 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. 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[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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