6e6m: Difference between revisions

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<StructureSection load='6e6m' size='340' side='right'caption='[[6e6m]], [[Resolution|resolution]] 1.55&Aring;' scene=''>
<StructureSection load='6e6m' size='340' side='right'caption='[[6e6m]], [[Resolution|resolution]] 1.55&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[6e6m]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6E6M OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6E6M FirstGlance]. <br>
<table><tr><td colspan='2'>[[6e6m]] is a 3 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=6E6M OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6E6M FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8CB:(1R,2R)-4,5-dimethyl-2-(prop-1-en-2-yl)-1,2,3,4-tetrahydro[1,1-biphenyl]-2,6-diol'>8CB</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.55&#8491;</td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">RBP1, CRBP1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8CB:(1R,2R)-4,5-dimethyl-2-(prop-1-en-2-yl)-1,2,3,4-tetrahydro[1,1-biphenyl]-2,6-diol'>8CB</scene></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=6e6m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e6m OCA], [http://pdbe.org/6e6m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6e6m RCSB], [http://www.ebi.ac.uk/pdbsum/6e6m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6e6m ProSAT]</span></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=6e6m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e6m OCA], [https://pdbe.org/6e6m PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6e6m RCSB], [https://www.ebi.ac.uk/pdbsum/6e6m PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6e6m ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/RET1_HUMAN RET1_HUMAN]] Intracellular transport of retinol.
[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.


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>
==See Also==
 
*[[Retinol-binding protein 3D structures|Retinol-binding protein 3D structures]]
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 6e6m" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Banerjee, S]]
[[Category: Banerjee S]]
[[Category: Golczak, M]]
[[Category: Golczak M]]
[[Category: Horwitz, S]]
[[Category: Horwitz S]]
[[Category: Kiser, P D]]
[[Category: Kiser PD]]
[[Category: Silvaroli, J A]]
[[Category: Silvaroli JA]]
[[Category: Cannabidiorcin]]
[[Category: Cbdo]]
[[Category: Lipid binding protein]]
[[Category: Retinol]]
[[Category: Vitamin some]]

Latest revision as of 17:39, 13 March 2024

Crystal structure of human cellular retinol-binding protein 1 in complex with cannabidiorcin (CBDO)Crystal structure of human cellular retinol-binding protein 1 in complex with cannabidiorcin (CBDO)

Structural highlights

6e6m is a 3 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.55Å
Ligands:
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

RET1_HUMAN Intracellular transport of retinol.

See Also

6e6m, resolution 1.55Å

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OCA
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