3fxv

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{{STRUCTURE_3fxv| PDB=3fxv | SCENE= }}
 
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===Identification of an N-oxide pyridine GW4064 analogue as a potent FXR agonist===
 
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{{ABSTRACT_PUBMED_19328688}}
 
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==Disease==
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==Identification of an N-oxide pyridine GW4064 analogue as a potent FXR agonist==
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[[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children.
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<StructureSection load='3fxv' size='340' side='right'caption='[[3fxv]], [[Resolution|resolution]] 2.26&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3fxv]] is a 2 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=3FXV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FXV FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.26&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=643:6-(4-{[3-(3,5-DICHLOROPYRIDIN-4-YL)-5-(1-METHYLETHYL)ISOXAZOL-4-YL]METHOXY}-2-METHYLPHENYL)-1-METHYL-1H-INDOLE-3-CARBOXYLIC+ACID'>643</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3fxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fxv OCA], [https://pdbe.org/3fxv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3fxv RCSB], [https://www.ebi.ac.uk/pdbsum/3fxv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3fxv ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref> <ref>PMID:10334993</ref> <ref>PMID:12815072</ref> <ref>PMID:15471871</ref> <ref>PMID:12718892</ref> <ref>PMID:18621523</ref> <ref>PMID:19410460</ref> <ref>PMID:19586769</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fx/3fxv_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3fxv ConSurf].
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<div style="clear:both"></div>
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==Function==
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==See Also==
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[[http://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN]] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref><ref>PMID:10334993</ref><ref>PMID:12815072</ref><ref>PMID:15471871</ref><ref>PMID:12718892</ref><ref>PMID:18621523</ref><ref>PMID:19410460</ref><ref>PMID:19586769</ref> [[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear receptors, such as for steroids (PGR, GR and ER), retinoids (RXRs), thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3, STAT5A, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors. Required with NCOA2 to control energy balance between white and brown adipose tissues. Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>PMID:9427757</ref><ref>PMID:7481822</ref><ref>PMID:9223431</ref><ref>PMID:9296499</ref><ref>PMID:9223281</ref><ref>PMID:10449719</ref><ref>PMID:12954634</ref>
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*[[Bile acid receptor 3D structures|Bile acid receptor 3D structures]]
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== References ==
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==About this Structure==
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<references/>
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[[3fxv]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FXV OCA].
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__TOC__
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</StructureSection>
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==Reference==
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<ref group="xtra">PMID:019328688</ref><references group="xtra"/><references/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Benson, G M.]]
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[[Category: Large Structures]]
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[[Category: Bleicher, K.]]
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[[Category: Benson GM]]
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[[Category: Chen, L.]]
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[[Category: Bleicher K]]
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[[Category: Feng, S.]]
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[[Category: Chen L]]
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[[Category: Grether, U.]]
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[[Category: Feng S]]
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[[Category: He, Y.]]
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[[Category: Grether U]]
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[[Category: Hong, D.]]
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[[Category: He Y]]
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[[Category: Kuhn, B.]]
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[[Category: Hong D]]
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[[Category: Martin, R.]]
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[[Category: Kuhn B]]
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[[Category: Plancher, J M.]]
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[[Category: Martin R]]
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[[Category: Richter, H.]]
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[[Category: Plancher J-M]]
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[[Category: Rudolph, M G.]]
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[[Category: Richter H]]
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[[Category: Wang, Z.]]
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[[Category: Rudolph MG]]
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[[Category: Yang, M.]]
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[[Category: Wang Z]]
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[[Category: Zhang, Z.]]
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[[Category: Yang M]]
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[[Category: Activator]]
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[[Category: Zhang Z]]
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[[Category: Acyltransferase]]
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[[Category: Bile acid]]
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[[Category: Cholesterol]]
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[[Category: Dna-binding]]
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[[Category: Hormone receptor]]
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[[Category: Metal-binding]]
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[[Category: Nuclear receptor]]
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[[Category: Nucleus]]
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[[Category: Phosphoprotein]]
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[[Category: Proto-oncogene]]
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[[Category: Receptor]]
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[[Category: Transcription]]
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[[Category: Transcription regulation]]
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[[Category: Transferase]]
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[[Category: Zinc-finger]]
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Current revision

Identification of an N-oxide pyridine GW4064 analogue as a potent FXR agonist

PDB ID 3fxv

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