AustralieFrV1, Main, Exploration, bibRecord, 001350

1α,20S-Dihydroxyvitamin D3 Interacts with Vitamin D Receptor: Crystal Structure and Route of Chemical Synthesis

Identifieur interne : 001350 ( Main/Exploration ); précédent : 001349; suivant : 001351

1α,20S-Dihydroxyvitamin D3 Interacts with Vitamin D Receptor: Crystal Structure and Route of Chemical Synthesis

Auteurs : Zongtao Lin [États-Unis] ; Hao Chen [États-Unis] ; Anna Y. Belorusova [France, Suède] ; John C. Bollinger [États-Unis] ; Edith K. Y. Tang ; Zorica Janjetovic [États-Unis] ; Tae-Kang Kim [États-Unis] ; Zhongzhi Wu [États-Unis] ; Duane D. Miller [États-Unis] ; Andrzej T. Slominski [États-Unis] ; Arnold E. Postlethwaite [États-Unis] ; Robert C. Tuckey ; Natacha Rochel [France] ; Wei Li [États-Unis]

Source :

Scientific Reports [ 2045-2322 ] ; 2017.

RBID : PMC:5579064

Abstract

1α,20S-Dihydroxyvitamin D3 [1,20S(OH)₂D₃], a natural and bioactive vitamin D3 metabolite, was chemically synthesized for the first time. X-ray crystallography analysis of intermediate 15 confirmed its 1α-OH configuration. 1,20S(OH)₂D₃ interacts with the vitamin D receptor (VDR), with similar potency to its native ligand, 1α,25-dihydroxyvitamin D₃ [1,25(OH)₂D₃] as illustrated by its ability to stimulate translocation of the VDR to the nucleus, stimulate VDRE-reporter activity, regulate VDR downstream genes (VDR, CYP24A1, TRPV6 and CYP27B1), and inhibit the production of inflammatory markers (IFNγ and IL1β). However, their co-crystal structures revealed differential molecular interactions of the 20S-OH moiety and the 25-OH moiety to the VDR, which may explain some differences in their biological activities. Furthermore, this study provides a synthetic route for the synthesis of 1,20S(OH)₂D₃ using the intermediate 1α,3β-diacetoxypregn-5-en-20-one (3), and provides a molecular and biological basis for the development of 1,20S(OH)₂D₃ and its analogs as potential therapeutic agents.

Url:

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5579064

DOI: 10.1038/s41598-017-10917-7
PubMed: 28860545
PubMed Central: 5579064

Affiliations:

France, Suède, États-Unis
Alabama, Tennessee

Le document en format XML

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-Dihydroxyvitamin D<sub>3</sub>
 Interacts with Vitamin D Receptor: Crystal Structure and Route of Chemical Synthesis</title>
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-Dihydroxyvitamin D<sub>3</sub>
 Interacts with Vitamin D Receptor: Crystal Structure and Route of Chemical Synthesis</title>
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<wicri:cityArea>Memphis</wicri:cityArea>
</affiliation>
</author>
<author><name sortKey="Slominski, Andrzej T" sort="Slominski, Andrzej T" uniqKey="Slominski A" first="Andrzej T." last="Slominski">Andrzej T. Slominski</name>
<affiliation wicri:level="2"><nlm:aff id="Aff5"><institution-wrap><institution-id institution-id-type="ISNI">0000000106344187</institution-id>
<institution-id institution-id-type="GRID">grid.265892.2</institution-id>
<institution>Department of Dermatology,</institution>
<institution>University of Alabama at Birmingham,</institution>
</institution-wrap>
Birmingham, AL 35294 United States</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<placeName><region type="state">Alabama</region>
</placeName>
<wicri:cityArea>Birmingham</wicri:cityArea>
</affiliation>
<affiliation wicri:level="2"><nlm:aff id="Aff6"><institution-wrap><institution-id institution-id-type="ISNI">0000 0004 0419 1326</institution-id>
<institution-id institution-id-type="GRID">grid.280808.a</institution-id>
<institution>VA Medical Center,</institution>
</institution-wrap>
Birmingham, AL 35294 United States</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<placeName><region type="state">Alabama</region>
</placeName>
<wicri:cityArea>Birmingham</wicri:cityArea>
</affiliation>
</author>
<author><name sortKey="Postlethwaite, Arnold E" sort="Postlethwaite, Arnold E" uniqKey="Postlethwaite A" first="Arnold E." last="Postlethwaite">Arnold E. Postlethwaite</name>
<affiliation wicri:level="2"><nlm:aff id="Aff7"><institution-wrap><institution-id institution-id-type="ISNI">0000 0004 0386 9246</institution-id>
<institution-id institution-id-type="GRID">grid.267301.1</institution-id>
<institution>Department of Medicine,</institution>
<institution>University of Tennessee Health Science Center,</institution>
</institution-wrap>
Memphis, TN 38163 United States</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<placeName><region type="state">Tennessee</region>
</placeName>
<wicri:cityArea>Memphis</wicri:cityArea>
</affiliation>
<affiliation wicri:level="2"><nlm:aff id="Aff8"><institution-wrap><institution-id institution-id-type="ISNI">0000 0004 0420 4721</institution-id>
<institution-id institution-id-type="GRID">grid.413847.d</institution-id>
<institution>VA Medical Center,</institution>
</institution-wrap>
Memphis, TN 38104 United States</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<placeName><region type="state">Tennessee</region>
</placeName>
<wicri:cityArea>Memphis</wicri:cityArea>
</affiliation>
</author>
<author><name sortKey="Tuckey, Robert C" sort="Tuckey, Robert C" uniqKey="Tuckey R" first="Robert C." last="Tuckey">Robert C. Tuckey</name>
<affiliation><nlm:aff id="Aff4"><institution-wrap><institution-id institution-id-type="ISNI">0000 0004 1936 7910</institution-id>
<institution-id institution-id-type="GRID">grid.1012.2</institution-id>
<institution>School of Chemistry and Biochemistry, University of Western Australia,</institution>
</institution-wrap>
Crawley, WA 6009 Australia</nlm:aff>
<wicri:noCountry code="subfield">WA 6009 Australia</wicri:noCountry>
</affiliation>
</author>
<author><name sortKey="Rochel, Natacha" sort="Rochel, Natacha" uniqKey="Rochel N" first="Natacha" last="Rochel">Natacha Rochel</name>
<affiliation wicri:level="1"><nlm:aff id="Aff2"><institution-wrap><institution-id institution-id-type="ISNI"> 0000 0004 0638 2716</institution-id>
<institution-id institution-id-type="GRID">grid.420255.4</institution-id>
<institution>Department of Integrative Structure Biology,</institution>
<institution>IGBMC - CNRS UMR7104 – Inserm U964, 1, rue Laurent Fries,</institution>
</institution-wrap>
Illkirch, 67400 France</nlm:aff>
<country xml:lang="fr">France</country>
<wicri:regionArea>Illkirch</wicri:regionArea>
</affiliation>
</author>
<author><name sortKey="Li, Wei" sort="Li, Wei" uniqKey="Li W" first="Wei" last="Li">Wei Li</name>
<affiliation wicri:level="2"><nlm:aff id="Aff1"><institution-wrap><institution-id institution-id-type="ISNI">0000 0004 0386 9246</institution-id>
<institution-id institution-id-type="GRID">grid.267301.1</institution-id>
<institution>Department of Pharmaceutical Sciences,</institution>
<institution>University of Tennessee Health Science Center, 881 Madison Avenue, Room 561,</institution>
</institution-wrap>
Memphis, TN 38163 United States</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<placeName><region type="state">Tennessee</region>
</placeName>
<wicri:cityArea>Memphis</wicri:cityArea>
</affiliation>
</author>
</analytic>
<series><title level="j">Scientific Reports</title>
<idno type="eISSN">2045-2322</idno>
<imprint><date when="2017">2017</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass></textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en"><p id="Par1">1α,20<italic>S</italic>
-Dihydroxyvitamin D3 [1,20<italic>S</italic>
(OH)<sub>2</sub>
D<sub>3</sub>
], a natural and bioactive vitamin D3 metabolite, was chemically synthesized for the first time. X-ray crystallography analysis of intermediate 15 confirmed its 1α-OH configuration. 1,20<italic>S</italic>
(OH)<sub>2</sub>
D<sub>3</sub>
 interacts with the vitamin D receptor (VDR), with similar potency to its native ligand, 1α,25-dihydroxyvitamin D<sub>3</sub>
 [1,25(OH)<sub>2</sub>
D<sub>3</sub>
] as illustrated by its ability to stimulate translocation of the VDR to the nucleus, stimulate VDRE-reporter activity, regulate VDR downstream genes (<italic>VDR</italic>
, <italic>CYP24A1</italic>
, <italic>TRPV6</italic>
 and <italic>CYP27B1</italic>
), and inhibit the production of inflammatory markers (IFNγ and IL1β). However, their co-crystal structures revealed differential molecular interactions of the 20<italic>S</italic>
-OH moiety and the 25-OH moiety to the VDR, which may explain some differences in their biological activities. Furthermore, this study provides a synthetic route for the synthesis of 1,20<italic>S</italic>
(OH)<sub>2</sub>
D<sub>3</sub>
 using the intermediate 1α,3β-diacetoxypregn-5-en-20-one (3), and provides a molecular and biological basis for the development of 1,20<italic>S</italic>
(OH)<sub>2</sub>
D<sub>3</sub>
 and its analogs as potential therapeutic agents.</p>
</div>
</front>
<back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Lin, Z" uniqKey="Lin Z">Z Lin</name>
</author>
<author><name sortKey="Li, W" uniqKey="Li W">W Li</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Wierzbicka, J" uniqKey="Wierzbicka J">J Wierzbicka</name>
</author>
<author><name sortKey="Piotrowska, A" uniqKey="Piotrowska A">A Piotrowska</name>
</author>
<author><name sortKey="Zmijewski, Ma" uniqKey="Zmijewski M">MA Zmijewski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Haussler, Mr" uniqKey="Haussler M">MR Haussler</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, At" uniqKey="Slominski A">AT Slominski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Li, W" uniqKey="Li W">W Li</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Tuckey, Rc" uniqKey="Tuckey R">RC Tuckey</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, At" uniqKey="Slominski A">AT Slominski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, At" uniqKey="Slominski A">AT Slominski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, At" uniqKey="Slominski A">AT Slominski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, At" uniqKey="Slominski A">AT Slominski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Lin, Z" uniqKey="Lin Z">Z Lin</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Lin, Z" uniqKey="Lin Z">Z Lin</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Lin, Z" uniqKey="Lin Z">Z Lin</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Wang, Q" uniqKey="Wang Q">Q Wang</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Yin, Yz" uniqKey="Yin Y">YZ Yin</name>
</author>
<author><name sortKey="Liu, C" uniqKey="Liu C">C Liu</name>
</author>
<author><name sortKey="Tang, Lq" uniqKey="Tang L">LQ Tang</name>
</author>
<author><name sortKey="Liu, Zp" uniqKey="Liu Z">ZP Liu</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Poza, J" uniqKey="Poza J">J Poza</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Mouri O, A" uniqKey="Mouri O A">A Mouriño</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Otero, R" uniqKey="Otero R">R Otero</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Huet, T" uniqKey="Huet T">T Huet</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, At" uniqKey="Slominski A">AT Slominski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="St Arnaud, R" uniqKey="St Arnaud R">R St-Arnaud</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Clapham, De" uniqKey="Clapham D">DE Clapham</name>
</author>
<author><name sortKey="Julius, D" uniqKey="Julius D">D Julius</name>
</author>
<author><name sortKey="Montell, C" uniqKey="Montell C">C Montell</name>
</author>
<author><name sortKey="Schultz, G" uniqKey="Schultz G">G Schultz</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Holick, Mf" uniqKey="Holick M">MF Holick</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Zbytek, B" uniqKey="Zbytek B">B Zbytek</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Pingili, Ak" uniqKey="Pingili A">AK Pingili</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Lin, Z" uniqKey="Lin Z">Z Lin</name>
</author>
<author><name sortKey="Yang, R" uniqKey="Yang R">R Yang</name>
</author>
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</author>
<author><name sortKey="Chen, A" uniqKey="Chen A">A Chen</name>
</author>
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</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Huet, T" uniqKey="Huet T">T Huet</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Otwinowski, Z" uniqKey="Otwinowski Z">Z Otwinowski</name>
</author>
<author><name sortKey="Minor, W" uniqKey="Minor W">W Minor</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Adams, Pd" uniqKey="Adams P">PD Adams</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Emsley, P" uniqKey="Emsley P">P Emsley</name>
</author>
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</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, A" uniqKey="Slominski A">A Slominski</name>
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</author>
<author><name sortKey="Slominski, R" uniqKey="Slominski R">R Slominski</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Kim, T K" uniqKey="Kim T">T-K Kim</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Slominski, At" uniqKey="Slominski A">AT Slominski</name>
</author>
</analytic>
</biblStruct>
</listBibl>
</div1>
</back>
</TEI>
<affiliations><list><country><li>France</li>
<li>Suède</li>
<li>États-Unis</li>
</country>
<region><li>Alabama</li>
<li>Tennessee</li>
</region>
</list>
<tree><noCountry><name sortKey="Tang, Edith K Y" sort="Tang, Edith K Y" uniqKey="Tang E" first="Edith K. Y." last="Tang">Edith K. Y. Tang</name>
<name sortKey="Tuckey, Robert C" sort="Tuckey, Robert C" uniqKey="Tuckey R" first="Robert C." last="Tuckey">Robert C. Tuckey</name>
</noCountry>
<country name="États-Unis"><region name="Tennessee"><name sortKey="Lin, Zongtao" sort="Lin, Zongtao" uniqKey="Lin Z" first="Zongtao" last="Lin">Zongtao Lin</name>
</region>
<name sortKey="Bollinger, John C" sort="Bollinger, John C" uniqKey="Bollinger J" first="John C." last="Bollinger">John C. Bollinger</name>
<name sortKey="Chen, Hao" sort="Chen, Hao" uniqKey="Chen H" first="Hao" last="Chen">Hao Chen</name>
<name sortKey="Janjetovic, Zorica" sort="Janjetovic, Zorica" uniqKey="Janjetovic Z" first="Zorica" last="Janjetovic">Zorica Janjetovic</name>
<name sortKey="Kim, Tae Kang" sort="Kim, Tae Kang" uniqKey="Kim T" first="Tae-Kang" last="Kim">Tae-Kang Kim</name>
<name sortKey="Li, Wei" sort="Li, Wei" uniqKey="Li W" first="Wei" last="Li">Wei Li</name>
<name sortKey="Miller, Duane D" sort="Miller, Duane D" uniqKey="Miller D" first="Duane D." last="Miller">Duane D. Miller</name>
<name sortKey="Postlethwaite, Arnold E" sort="Postlethwaite, Arnold E" uniqKey="Postlethwaite A" first="Arnold E." last="Postlethwaite">Arnold E. Postlethwaite</name>
<name sortKey="Postlethwaite, Arnold E" sort="Postlethwaite, Arnold E" uniqKey="Postlethwaite A" first="Arnold E." last="Postlethwaite">Arnold E. Postlethwaite</name>
<name sortKey="Slominski, Andrzej T" sort="Slominski, Andrzej T" uniqKey="Slominski A" first="Andrzej T." last="Slominski">Andrzej T. Slominski</name>
<name sortKey="Slominski, Andrzej T" sort="Slominski, Andrzej T" uniqKey="Slominski A" first="Andrzej T." last="Slominski">Andrzej T. Slominski</name>
<name sortKey="Wu, Zhongzhi" sort="Wu, Zhongzhi" uniqKey="Wu Z" first="Zhongzhi" last="Wu">Zhongzhi Wu</name>
</country>
<country name="France"><noRegion><name sortKey="Belorusova, Anna Y" sort="Belorusova, Anna Y" uniqKey="Belorusova A" first="Anna Y." last="Belorusova">Anna Y. Belorusova</name>
</noRegion>
<name sortKey="Rochel, Natacha" sort="Rochel, Natacha" uniqKey="Rochel N" first="Natacha" last="Rochel">Natacha Rochel</name>
</country>
<country name="Suède"><noRegion><name sortKey="Belorusova, Anna Y" sort="Belorusova, Anna Y" uniqKey="Belorusova A" first="Anna Y." last="Belorusova">Anna Y. Belorusova</name>
</noRegion>
</country>
</tree>
</affiliations>
</record>

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1α,20S-Dihydroxyvitamin D3 Interacts with Vitamin D Receptor: Crystal Structure and Route of Chemical Synthesis

1α,20S-Dihydroxyvitamin D3 Interacts with Vitamin D Receptor: Crystal Structure and Route of Chemical Synthesis

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