3fc6
From Proteopedia
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- | [[ | + | ==hRXRalpha & mLXRalpha with an indole Pharmacophore, SB786875== |
+ | <StructureSection load='3fc6' size='340' side='right' caption='[[3fc6]], [[Resolution|resolution]] 2.06Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[3fc6]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FC6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3FC6 FirstGlance]. <br> | ||
+ | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LX2:[4-(3-{[2-CHLORO-3-(TRIFLUOROMETHYL)BENZYL](2,2-DIPHENYLETHYL)AMINO}PROPOXY)-1H-INDOL-1-YL]ACETIC+ACID'>LX2</scene>, <scene name='pdbligand=REA:RETINOIC+ACID'>REA</scene><br> | ||
+ | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3fc6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fc6 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3fc6 RCSB], [http://www.ebi.ac.uk/pdbsum/3fc6 PDBsum]</span></td></tr> | ||
+ | <table> | ||
+ | == Evolutionary Conservation == | ||
+ | [[Image:Consurf_key_small.gif|200px|right]] | ||
+ | Check<jmol> | ||
+ | <jmolCheckbox> | ||
+ | <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fc/3fc6_consurf.spt"</scriptWhenChecked> | ||
+ | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
+ | <text>to colour the structure by Evolutionary Conservation</text> | ||
+ | </jmolCheckbox> | ||
+ | </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/chain_selection.php?pdb_ID=2ata ConSurf]. | ||
+ | <div style="clear:both"></div> | ||
+ | <div style="background-color:#fffaf0;"> | ||
+ | == Publication Abstract from PubMed == | ||
+ | A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRalpha will be disclosed. | ||
- | + | Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.,Washburn DG, Hoang TH, Campobasso N, Smallwood A, Parks DJ, Webb CL, Frank KA, Nord M, Duraiswami C, Evans C, Jaye M, Thompson SK Bioorg Med Chem Lett. 2009 Jan 9. PMID:19167885<ref>PMID:19167885</ref> | |
- | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
- | + | </div> | |
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==See Also== | ==See Also== | ||
*[[Retinoid X receptor|Retinoid X receptor]] | *[[Retinoid X receptor|Retinoid X receptor]] | ||
- | + | == References == | |
- | == | + | <references/> |
- | < | + | __TOC__ |
+ | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Mus musculus]] | [[Category: Mus musculus]] |
Revision as of 13:29, 29 September 2014
hRXRalpha & mLXRalpha with an indole Pharmacophore, SB786875
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Categories: Homo sapiens | Mus musculus | Campobasso, N. | Duraiswami, C. | Evans, C. | Frank, K. | Hoang, T H. | Jaye, M. | Nord, M. | Parks, D J. | Smallwood, A. | Thompson, S K. | Washburn, D G. | Webb, C L. | Agonist | Dna-binding | Epoxycholesterol | Host-virus interaction | Liver x receptor | Metal-binding | Nuclear hormone receptor | Nucleus | Receptor | Transcription | Transcription regulation | Zinc-finger