1r6g

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[[Image:1r6g.gif|left|200px]]
 
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==Crystal structure of the thyroid hormone receptor beta ligand binding domain in complex with a beta selective compound==
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The line below this paragraph, containing "STRUCTURE_1r6g", creates the "Structure Box" on the page.
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<StructureSection load='1r6g' size='340' side='right'caption='[[1r6g]], [[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'>[[1r6g]] 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=1R6G OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1R6G 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]] 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=442:2-[3,5-DIBROMO-4-(4-HYDROXY-3-{HYDROXY[(2-PHENYLETHYL)AMINO]METHYL}PHENOXY)PHENYL]ETHANE-1,1-DIOL'>442</scene></td></tr>
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{{STRUCTURE_1r6g| PDB=1r6g | 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=1r6g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r6g OCA], [https://pdbe.org/1r6g PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1r6g RCSB], [https://www.ebi.ac.uk/pdbsum/1r6g PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1r6g ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/THB_HUMAN THB_HUMAN] Defects in THRB are the cause of generalized thyroid hormone resistance (GTHR) [MIM:[https://omim.org/entry/188570 188570]. GTHR is a disease characterized by goiter, abnormal mental functions, increased susceptibility to infections, abnormal growth and bone maturation, tachycardia and deafness. Affected individuals may also have attention deficit-hyperactivity disorders (ADHD) and language difficulties. GTHR patients also have high levels of circulating thyroid hormones (T3-T4), with normal or slightly elevated thyroid stimulating hormone (TSH).<ref>PMID:2510172</ref> <ref>PMID:2153155</ref> <ref>PMID:1846005</ref> <ref>PMID:1661299</ref> <ref>PMID:1653889</ref> <ref>PMID:1563081</ref> <ref>PMID:1314846</ref> <ref>PMID:1619012</ref> <ref>PMID:1587388</ref> <ref>PMID:1324420</ref> <ref>PMID:8514853</ref> <ref>PMID:8175986</ref> <ref>PMID:7833659</ref> <ref>PMID:8664910</ref> <ref>PMID:8889584</ref> <ref>PMID:10660344</ref> <ref>PMID:16804041</ref> <ref>PMID:19268523</ref> Defects in THRB are the cause of generalized thyroid hormone resistance autosomal recessive (GTHRAR) [MIM:[https://omim.org/entry/274300 274300]. An autosomal recessive disorder characterized by goiter, clinical euthyroidism, end-organ unresponsiveness to thyroid hormone, abnormal growth and bone maturation, and deafness. Patients also have high levels of circulating thyroid hormones, with elevated thyroid stimulating hormone. Defects in THRB are the cause of selective pituitary thyroid hormone resistance (PRTH) [MIM:[https://omim.org/entry/145650 145650]; also known as familial hyperthyroidism due to inappropriate thyrotropin secretion. PRTH is a variant form of thyroid hormone resistance and is characterized by clinical hyperthyroidism, with elevated free thyroid hormones, but inappropriately normal serum TSH. Unlike GRTH, where the syndrome usually segregates with a dominant allele, the mode of inheritance in PRTH has not been established.<ref>PMID:7528740</ref> <ref>PMID:8381821</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/THB_HUMAN THB_HUMAN] High affinity receptor for triiodothyronine.<ref>PMID:17418816</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/r6/1r6g_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=1r6g ConSurf].
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<div style="clear:both"></div>
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'''Crystal structure of the thyroid hormone receptor beta ligand binding domain in complex with a beta selective compound'''
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==See Also==
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*[[Thyroid hormone receptor 3D structures|Thyroid hormone receptor 3D structures]]
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== References ==
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==Overview==
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<references/>
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A set of thyromimetics having improved selectivity for TR-beta1 were prepared by replacing the 3'-isopropyl group of 2 and 3 with substituents having increased steric bulk. From this limited SAR study, the most potent and selective compounds identified were derived from 2 and contained a 3'-phenyl moiety bearing small hydrophobic groups meta to the biphenyl link. X-ray crystal data of 15c complexed with TR-beta1 LBD shows methionine 442 to be displaced by the bulky R3' phenyl ethyl amide side chain. Movement of this amino acid side chain provides an expanded pocket for the bulky side chain while the ligand-receptor complex retains full agonist activity.
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__TOC__
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</StructureSection>
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==About this Structure==
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1R6G 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=1R6G OCA].
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==Reference==
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Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta., Hangeland JJ, Doweyko AM, Dejneka T, Friends TJ, Devasthale P, Mellstrom K, Sandberg J, Grynfarb M, Sack JS, Einspahr H, Farnegardh M, Husman B, Ljunggren J, Koehler K, Sheppard C, Malm J, Ryono DE, Bioorg Med Chem Lett. 2004 Jul 5;14(13):3549-53. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15177471 15177471]
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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: Dejneka, T.]]
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[[Category: Dejneka T]]
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[[Category: Devasthale, P.]]
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[[Category: Devasthale P]]
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[[Category: Doweyko, A M.]]
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[[Category: Doweyko AM]]
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[[Category: Einspahr, H.]]
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[[Category: Einspahr H]]
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[[Category: Farnegardh, M.]]
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[[Category: Farnegardh M]]
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[[Category: Friends, T J.]]
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[[Category: Friends TJ]]
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[[Category: Grynfarb, M.]]
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[[Category: Grynfarb M]]
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[[Category: Hangeland, J J.]]
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[[Category: Hangeland JJ]]
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[[Category: Husman, B.]]
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[[Category: Husman B]]
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[[Category: Koehler, K.]]
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[[Category: Koehler K]]
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[[Category: Ljunggren, J.]]
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[[Category: Ljunggren J]]
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[[Category: Malm, J.]]
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[[Category: Malm J]]
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[[Category: Mellstrom, K.]]
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[[Category: Mellstrom K]]
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[[Category: Ryono, D E.]]
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[[Category: Ryono DE]]
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[[Category: Sack, J S.]]
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[[Category: Sack JS]]
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[[Category: Sandberg, J.]]
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[[Category: Sandberg J]]
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[[Category: Sheppard, C.]]
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[[Category: Sheppard C]]
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[[Category: Alpha helical]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:08:36 2008''
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Current revision

Crystal structure of the thyroid hormone receptor beta ligand binding domain in complex with a beta selective compound

PDB ID 1r6g

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