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5lga

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Revision as of 18:37, 15 November 2017

Structural analysis and biological activities of BXL0124, a Gemini analog of Vitamin D

Structural highlights

5lga is a 2 chain structure with sequence from Brachidanio rerio. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Gene:	vdra, nr1i1a, vdr (Brachidanio rerio)
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[VDRA_DANRE] Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis.^[1]

Publication Abstract from PubMed

Gemini analogs of calcitriol, characterized by the extension of the C21-methyl group of calcitriol with a second chain, act as agonists of the vitamin D receptor (VDR). This second side chain of gemini is accommodated in a new cavity inside the VDR created by the structural rearrangement of the protein core. The resulting conformational change preserves the active state of the receptor and bestows gemini compounds with biological activities that exceed those of calcitriol. Of particular interest are gemini's anti-cancer properties, and in this study we demonstrate anti-proliferative and tumor-reducing abilities of BXL0124 and BXL0097, differing only by the presence or absence, respectively, of the methylene group on the A ring. BXL0124 acts as a more potent VDR agonist than its 19-nor counterpart by activating VDR-mediated transcription at lower concentrations. In a similar manner, BXL0124 is more active than BXL0097 in growth inhibition of breast cancer cells and reduction of tumor volume. Structural comparisons of BXL0097 and BXL0124, as their VDR complexes, explain the elevated activity of the latter.

Structural analysis and biological activities of BXL0124, a gemini analog of vitamin D.,Belorusova AY, Suh N, Lee HJ, So JY, Maehr H, Rochel N J Steroid Biochem Mol Biol. 2016 Sep 17. pii: S0960-0760(16)30251-5. doi:, 10.1016/j.jsbmb.2016.09.015. PMID:27650654^[2]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Ciesielski F, Rochel N, Moras D. Adaptability of the Vitamin D nuclear receptor to the synthetic ligand Gemini: remodelling the LBP with one side chain rotation. J Steroid Biochem Mol Biol. 2007 Mar;103(3-5):235-42. Epub 2007 Jan 10. PMID:17218092 doi:http://dx.doi.org/10.1016/j.jsbmb.2006.12.003
↑ Belorusova AY, Suh N, Lee HJ, So JY, Maehr H, Rochel N. Structural analysis and biological activities of BXL0124, a gemini analog of vitamin D. J Steroid Biochem Mol Biol. 2016 Sep 17. pii: S0960-0760(16)30251-5. doi:, 10.1016/j.jsbmb.2016.09.015. PMID:27650654 doi:http://dx.doi.org/10.1016/j.jsbmb.2016.09.015

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/5lga"

@@ Line 3: / Line 3: @@
 <StructureSection load='5lga' size='340' side='right' caption='[[5lga]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[5lga]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LGA FirstGlance]. <br>
+<table><tr><td colspan='2'>[[5lga]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Brachidanio_rerio Brachidanio rerio]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LGA FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6VH:(1~{R},3~{S},5~{Z})-5-[2-[(1~{R},3~{A}~{S},7~{A}~{R})-7~{A}-METHYL-1-[(6~{R})-1,1,1-TRIS(FLUORANYL)-10-METHYL-2,10-BIS(OXIDANYL)-2-(TRIFLUOROMETHYL)UNDECA-3,8-DIYN-6-YL]-2,3,3~{A},5,6,7-HEXAHYDRO-1~{H}-INDEN-4-YLIDENE]ETHYLIDENE]-4-METHYLIDENE-CYCLOHEXANE-1,3-DIOL'>6VH</scene></td></tr>
+<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">vdra, nr1i1a, vdr ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=7955 Brachidanio rerio])</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=5lga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lga OCA], [http://pdbe.org/5lga PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lga RCSB], [http://www.ebi.ac.uk/pdbsum/5lga PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lga ProSAT]</span></td></tr>
 </table>
@@ Line 22: / Line 23: @@
 __TOC__
 </StructureSection>
+[[Category: Brachidanio rerio]]
 [[Category: Belorusova, A Y]]
 [[Category: Rochel, N]]

5lga

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Revision as of 18:37, 15 November 2017

Structural analysis and biological activities of BXL0124, a Gemini analog of Vitamin D

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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