1nde

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{{Seed}}
 
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[[Image:1nde.png|left|200px]]
 
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==Estrogen Receptor beta with Selective Triazine Modulator==
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The line below this paragraph, containing "STRUCTURE_1nde", creates the "Structure Box" on the page.
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<StructureSection load='1nde' size='340' side='right'caption='[[1nde]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[1nde]] is a 1 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=1NDE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1NDE FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 3&#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=MON:4-(2-{[4-{[3-(4-CHLOROPHENYL)PROPYL]SULFANYL}-6-(1-PIPERAZINYL)-1,3,5-TRIAZIN-2-YL]AMINO}ETHYL)PHENOL'>MON</scene></td></tr>
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{{STRUCTURE_1nde| PDB=1nde | SCENE= }}
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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=1nde FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1nde OCA], [https://pdbe.org/1nde PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1nde RCSB], [https://www.ebi.ac.uk/pdbsum/1nde PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1nde ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.
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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/nd/1nde_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=1nde ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A series of 1,3,5-triazine-based estrogen receptor (ER) modulators that are modestly selective for the ERbeta subtype are reported. Compound 1, which displayed modest potency and selectivity for ERbeta vs ERalpha, was identified via high-throughput screening utilizing an ERbeta SPA-based binding assay. Subsequent analogue preparation resulted in the identification of compounds such as 21 and 43 that display 25- to 30-fold selectivity for ERbeta with potencies in the 10-30 nM range. These compounds profile as full antagonists at ERbeta and weak partial agonists at ERalpha in a cell-based reporter gene assay. In addition, the X-ray crystal structure of compound 15 complexed with the ligand binding domain of ERbeta has been solved and was utilized in the design of more conformationally restrained analogues such as 31 in an attempt to increase selectivity for the ERbeta subtype.
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===Estrogen Receptor beta with Selective Triazine Modulator===
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A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.,Henke BR, Consler TG, Go N, Hale RL, Hohman DR, Jones SA, Lu AT, Moore LB, Moore JT, Orband-Miller LA, Robinett RG, Shearin J, Spearing PK, Stewart EL, Turnbull PS, Weaver SL, Williams SP, Wisely GB, Lambert MH J Med Chem. 2002 Dec 5;45(25):5492-505. PMID:12459017<ref>PMID:12459017</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 1nde" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_12459017}}, adds the Publication Abstract to the page
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*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 12459017 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_12459017}}
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__TOC__
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</StructureSection>
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==About this Structure==
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1NDE is a [[Single protein]] structure of 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=1NDE OCA].
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==Reference==
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A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta., Henke BR, Consler TG, Go N, Hale RL, Hohman DR, Jones SA, Lu AT, Moore LB, Moore JT, Orband-Miller LA, Robinett RG, Shearin J, Spearing PK, Stewart EL, Turnbull PS, Weaver SL, Williams SP, Wisely GB, Lambert MH, J Med Chem. 2002 Dec 5;45(25):5492-505. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12459017 12459017]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Single protein]]
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[[Category: Large Structures]]
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[[Category: Consler, T G.]]
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[[Category: Consler TG]]
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[[Category: Go, N.]]
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[[Category: Go N]]
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[[Category: Hale, R L.]]
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[[Category: Hale RL]]
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[[Category: Henke, B R.]]
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[[Category: Henke BR]]
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[[Category: Hohman, D R.]]
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[[Category: Hohman DR]]
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[[Category: Jones, S A.]]
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[[Category: Jones SA]]
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[[Category: Lambert, M H.]]
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[[Category: Lambert MH]]
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[[Category: Lu, A T.]]
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[[Category: Lu AT]]
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[[Category: Moore, J T.]]
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[[Category: Moore JT]]
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[[Category: Moore, L B.]]
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[[Category: Moore LB]]
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[[Category: Orband-Miller, L A.]]
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[[Category: Orband-Miller LA]]
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[[Category: Robinett, R G.]]
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[[Category: Robinett RG]]
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[[Category: Shearin, J.]]
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[[Category: Shearin J]]
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[[Category: Spearing, P K.]]
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[[Category: Spearing PK]]
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[[Category: Stewart, E L.]]
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[[Category: Stewart EL]]
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[[Category: Turnbull, P S.]]
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[[Category: Turnbull PS]]
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[[Category: Weaver, S L.]]
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[[Category: Weaver SL]]
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[[Category: Williams, S P.]]
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[[Category: Williams SP]]
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[[Category: Wisely, G B.]]
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[[Category: Wisely GB]]
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[[Category: Er]]
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[[Category: Erb]]
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[[Category: Estradiol]]
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[[Category: Estrogen]]
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[[Category: Estrogen receptor]]
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[[Category: Estrogen receptor beta]]
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[[Category: Oestrogen]]
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[[Category: Triazine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 17:28:30 2008''
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Current revision

Estrogen Receptor beta with Selective Triazine Modulator

PDB ID 1nde

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