3hf6
From Proteopedia
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==Crystal structure of human tryptophan hydroxylase type 1 with bound LP-521834 and FE== | ==Crystal structure of human tryptophan hydroxylase type 1 with bound LP-521834 and FE== | ||
| - | <StructureSection load='3hf6' size='340' side='right' caption='[[3hf6]], [[Resolution|resolution]] 1.80Å' scene=''> | + | <StructureSection load='3hf6' size='340' side='right'caption='[[3hf6]], [[Resolution|resolution]] 1.80Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[3hf6]] is a 1 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[3hf6]] 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=3HF6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3HF6 FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FE:FE+(III)+ION'>FE</scene>, <scene name='pdbligand=LX0:4-(4-AMINO-6-{[(1R)-1-NAPHTHALEN-2-YLETHYL]AMINO}-1,3,5-TRIAZIN-2-YL)-L-PHENYLALANINE'>LX0</scene | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.8Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FE:FE+(III)+ION'>FE</scene>, <scene name='pdbligand=LX0:4-(4-AMINO-6-{[(1R)-1-NAPHTHALEN-2-YLETHYL]AMINO}-1,3,5-TRIAZIN-2-YL)-L-PHENYLALANINE'>LX0</scene></td></tr> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3hf6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3hf6 OCA], [https://pdbe.org/3hf6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3hf6 RCSB], [https://www.ebi.ac.uk/pdbsum/3hf6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3hf6 ProSAT]</span></td></tr> |
</table> | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/TPH1_HUMAN TPH1_HUMAN] | ||
== Evolutionary Conservation == | == Evolutionary Conservation == | ||
[[Image:Consurf_key_small.gif|200px|right]] | [[Image:Consurf_key_small.gif|200px|right]] | ||
Check<jmol> | Check<jmol> | ||
<jmolCheckbox> | <jmolCheckbox> | ||
| - | <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/hf/3hf6_consurf.spt"</scriptWhenChecked> | + | <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/hf/3hf6_consurf.spt"</scriptWhenChecked> |
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
<text>to colour the structure by Evolutionary Conservation</text> | <text>to colour the structure by Evolutionary Conservation</text> | ||
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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=3hf6 ConSurf]. | </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=3hf6 ConSurf]. | ||
<div style="clear:both"></div> | <div style="clear:both"></div> | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. As a neurotransmitter, serotonin plays important physiological roles both peripherally and centrally. Here we describe the discovery of substituted triazines as a novel class of tryptophan hydroxylase inhibitors. This class of TPH inhibitors can selectively reduce serotonin levels in murine intestine after oral administration without affecting levels in the brain. These TPH inhibitors may provide novel treatments for gastrointestinal disorders associated with dysregulation of the serotonergic system, such as chemotherapy-induced emesis and irritable bowel syndrome. | ||
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| - | Substituted 3-(4-(1,3,5-triazin-2-yl)-phenyl)-2-aminopropanoic acids as novel tryptophan hydroxylase inhibitors.,Jin H, Cianchetta G, Devasagayaraj A, Gu K, Marinelli B, Samala L, Scott S, Stouch T, Tunoori A, Wang Y, Zang Y, Zhang C, David Kimball S, Main AJ, Ding ZM, Sun W, Yang Q, Yu XQ, Powell DR, Wilson A, Liu Q, Shi ZC Bioorg Med Chem Lett. 2009 Sep 1;19(17):5229-32. Epub 2009 Jul 8. PMID:19631532<ref>PMID:19631532</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 3hf6" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
| - | *[[ | + | *[[Hydroxylases 3D structures|Hydroxylases 3D structures]] |
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: Hunter | + | [[Category: Hunter MJ]] |
| - | [[Category: Swanson | + | [[Category: Swanson RV]] |
| - | [[Category: Tari | + | [[Category: Tari LW]] |
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Current revision
Crystal structure of human tryptophan hydroxylase type 1 with bound LP-521834 and FE
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