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4whf

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Revision as of 21:32, 15 October 2015

Crystal Structure of TR3 LBD in complex with 1-(3,4,5-trihydroxyphenyl)decan-1-one

Structural highlights

4whf is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Related:	4whg, 4re8, 4ree, 4ref
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum

Function

[NR4A1_HUMAN] Orphan nuclear receptor. May act concomitantly with NURR1 in regulating the expression of delayed-early genes during liver regeneration. Binds the NGFI-B response element (NBRE) 5'-AAAAGGTCA-3' (By similarity). May inhibit NF-kappa-B transactivation of IL2.^[1]

Publication Abstract from PubMed

Apoptotic resistance is becoming a significant obstacle for cancer therapy as the majority of treatment takes the route of apoptotic induction. It is of great importance to develop an alternative strategy to induce cancer cell death. We previously reported that autophagic cell death mediated by nuclear receptor TR3 and driven by a chemical agonist, 1-(3,4,5-trihydroxyphenyl)nonan-1-one (THPN), is highly effective in the therapy of melanoma but not any other cancer types. Here, we discovered that the insensitivity of cancer cells to THPN originated from a high cellular Akt2 activity. Akt2 phosphorylation interferes with TR3 export to cytoplasm and targeting to mitochondria, which lead to the autophagic induction. Therefore, the TR3-mediated autophagy could be effectively induced in the otherwise insensitive cells by downregulating Akt2 activity. Highly effective antineoplastic compounds are developed through optimizing the structure of THPN. This study implicates a general strategy for cancer therapy by the induction of autophagic cell death.

Induction of Autophagic Death in Cancer Cells by Agonizing TR3 and Attenuating Akt2 Activity.,Wang WJ, Wang Y, Hou PP, Li FW, Zhou B, Chen HZ, Bian XL, Cai QX, Xing YZ, He JP, Zhang H, Huang PQ, Lin T, Wu Q Chem Biol. 2015 Aug 20;22(8):1040-51. doi: 10.1016/j.chembiol.2015.06.023. Epub, 2015 Jul 30. PMID:26235054^[2]

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

References

↑ Harant H, Lindley IJ. Negative cross-talk between the human orphan nuclear receptor Nur77/NAK-1/TR3 and nuclear factor-kappaB. Nucleic Acids Res. 2004 Oct 5;32(17):5280-90. Print 2004. PMID:15466594 doi:10.1093/nar/gkh856
↑ Wang WJ, Wang Y, Hou PP, Li FW, Zhou B, Chen HZ, Bian XL, Cai QX, Xing YZ, He JP, Zhang H, Huang PQ, Lin T, Wu Q. Induction of Autophagic Death in Cancer Cells by Agonizing TR3 and Attenuating Akt2 Activity. Chem Biol. 2015 Aug 20;22(8):1040-51. doi: 10.1016/j.chembiol.2015.06.023. Epub, 2015 Jul 30. PMID:26235054 doi:http://dx.doi.org/10.1016/j.chembiol.2015.06.023

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/4whf"

@@ Line 5: / Line 5: @@
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3MX:1-(3,4,5-TRIHYDROXYPHENYL)DECAN-1-ONE'>3MX</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4whg|4whg]], [[4re8|4re8]], [[4ree|4ree]], [[4ref|4ref]]</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=4whf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4whf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4whf RCSB], [http://www.ebi.ac.uk/pdbsum/4whf PDBsum]</span></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=4whf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4whf OCA], [http://pdbe.org/4whf PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4whf RCSB], [http://www.ebi.ac.uk/pdbsum/4whf PDBsum]</span></td></tr>
 </table>
 == Function ==
@@ Line 17: / Line 17: @@
 From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 </div>
+<div class="pdbe-citations 4whf" style="background-color:#fffaf0;"></div>
 == References ==
 <references/>

4whf

From Proteopedia

Revision as of 21:32, 15 October 2015

Crystal Structure of TR3 LBD in complex with 1-(3,4,5-trihydroxyphenyl)decan-1-one

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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