7zij - Revision history

OCA at 13:32, 1 February 2024

OCA — Thu, 01 Feb 2024 13:32:27 GMT

←Older revision		Revision as of 13:32, 1 February 2024
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[7zij]] 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=7ZIJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7ZIJ FirstGlance]. <br>		<table><tr><td colspan='2'>[[7zij]] 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=7ZIJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7ZIJ FirstGlance]. <br>
-	</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=IVW:8-(1~{H}-benzimidazol-2-ylmethyl)-3-cyclopropyl-7-(phenylmethyl)purine-2,6-dione'>IVW</scene></td></tr>	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 1.9467837Å</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=IVW:8-(1~{H}-benzimidazol-2-ylmethyl)-3-cyclopropyl-7-(phenylmethyl)purine-2,6-dione'>IVW</scene></td></tr>
	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7zij FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7zij OCA], [https://pdbe.org/7zij PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7zij RCSB], [https://www.ebi.ac.uk/pdbsum/7zij PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7zij ProSAT]</span></td></tr>		<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7zij FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7zij OCA], [https://pdbe.org/7zij PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7zij RCSB], [https://www.ebi.ac.uk/pdbsum/7zij PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7zij ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/TPH1_HUMAN TPH1_HUMAN]]	+	[https://www.uniprot.org/uniprot/TPH1_HUMAN TPH1_HUMAN]
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</div>		</div>
	<div class="pdbe-citations 7zij" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 7zij" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Hydroxylases 3D structures\|Hydroxylases 3D structures]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 18:46, 7 September 2022

OCA — Wed, 07 Sep 2022 18:46:15 GMT

←Older revision		Revision as of 18:46, 7 September 2022
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	== Function ==		== Function ==
	[[https://www.uniprot.org/uniprot/TPH1_HUMAN TPH1_HUMAN]]		[[https://www.uniprot.org/uniprot/TPH1_HUMAN TPH1_HUMAN]]
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Tryptophan hydroxylases catalyze the first and rate-limiting step in the synthesis of serotonin. Serotonin is a key neurotransmitter in the central nervous system and, in the periphery, functions as a local hormone with multiple physiological functions. Studies in genetically altered mouse models have shown that dysregulation of peripheral serotonin levels leads to metabolic, inflammatory, and fibrotic diseases. Overproduction of serotonin by tumor cells causes severe symptoms typical for the carcinoid syndrome, and tryptophan hydroxylase inhibitors are already in clinical use for patients suffering from this disease. Here, we describe a novel class of potent tryptophan hydroxylase inhibitors, characterized by spanning all active binding sites important for catalysis, specifically those of the cosubstrate pterin, the substrate tryptophan as well as directly chelating the catalytic iron ion. The inhibitors were designed to efficiently reduce serotonin in the periphery while not passing the blood-brain barrier, thus preserving serotonin levels in the brain.
		+
		+	Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors.,Specker E, Matthes S, Wesolowski R, Schutz A, Grohmann M, Alenina N, Pleimes D, Mallow K, Neuenschwander M, Gogolin A, Weise M, Pfeifer J, Ziebart N, Heinemann U, von Kries JP, Nazare M, Bader M J Med Chem. 2022 Aug 25;65(16):11126-11149. doi: 10.1021/acs.jmedchem.2c00598., Epub 2022 Aug 3. PMID:35921615<ref>PMID:35921615</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7zij" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>

OCA at 16:41, 7 September 2022

OCA — Wed, 07 Sep 2022 16:41:05 GMT

←Older revision		Revision as of 16:41, 7 September 2022
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-	'''Unreleased structure'''

-	~~The entry~~ 7zij is ~~ON HOLD until Paper Publication~~	+	==Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor KM-05-080==
-		+	<StructureSection load='7zij' size='340' side='right'caption='[[7zij]], [[Resolution\|resolution]] 1.95Å' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[7zij]] 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=7ZIJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7ZIJ FirstGlance]. <br>
-	~~Description~~:	+	</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=IVW:8-(1~{H}-benzimidazol-2-ylmethyl)-3-cyclopropyl-7-(phenylmethyl)purine-2,6-dione'>IVW</scene></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7zij FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7zij OCA], [https://pdbe.org/7zij PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7zij RCSB], [https://www.ebi.ac.uk/pdbsum/7zij PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7zij ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[https://www.uniprot.org/uniprot/TPH1_HUMAN TPH1_HUMAN]]
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Homo sapiens]]
		+	[[Category: Large Structures]]
		+	[[Category: Heinemann U]]
		+	[[Category: Mallow K]]
		+	[[Category: Nazare M]]
		+	[[Category: Schuetz A]]
		+	[[Category: Specker E]]

OCA at 04:01, 15 June 2022

OCA — Wed, 15 Jun 2022 04:01:58 GMT

←Older revision		Revision as of 04:01, 15 June 2022
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7zij is ON HOLD	+	The entry 7zij is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "7zij" [edit=sysop:move=sysop]

OCA — Wed, 13 Apr 2022 08:51:51 GMT

Protected "7zij" [edit=sysop:move=sysop]

←Older revision

Revision as of 08:51, 13 April 2022

OCA: New page: '''Unreleased structure''' The entry 7zij is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 13 Apr 2022 08:51:51 GMT

New page: '''Unreleased structure''' The entry 7zij is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7zij is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]