5n3w - Revision history

OCA at 18:01, 8 November 2023

OCA — Wed, 08 Nov 2023 18:01:02 GMT

←Older revision		Revision as of 18:01, 8 November 2023
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	<StructureSection load='5n3w' size='340' side='right'caption='[[5n3w]], [[Resolution\|resolution]] 2.30Å' scene=''>		<StructureSection load='5n3w' size='340' side='right'caption='[[5n3w]], [[Resolution\|resolution]] 2.30Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5n3w]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5N3W OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5N3W FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5n3w]] 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=5N3W OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5N3W FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8KW:3-[2-(2-HYDROXYPHENYL)ETHYL]-5-METHOXY-PHENOL'>8KW</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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]] 2.3Å</td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Leukotriene-A(4)_hydrolase Leukotriene-A(4) hydrolase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.3.2.6 3.3.2.6] </span></td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8KW:3-[2-(2-HYDROXYPHENYL)ETHYL]-5-METHOXY-PHENOL'>8KW</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://proteopedia.org/fgij/fg.htm?mol=5n3w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5n3w OCA], [~~http~~://pdbe.org/5n3w PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5n3w RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5n3w PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5n3w 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=5n3w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5n3w OCA], [https://pdbe.org/5n3w PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5n3w RCSB], [https://www.ebi.ac.uk/pdbsum/5n3w PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5n3w ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/LKHA4_HUMAN LKHA4_HUMAN]] Epoxide hydrolase that catalyzes the final step in the biosynthesis of the proinflammatory mediator leukotriene B4. Has also aminopeptidase activity.<ref>PMID:1897988</ref> <ref>PMID:1975494</ref> <ref>PMID:2244921</ref> <ref>PMID:12207002</ref> <ref>PMID:11917124</ref> <ref>PMID:15078870</ref> <ref>PMID:18804029</ref>	+	[https://www.uniprot.org/uniprot/LKHA4_HUMAN LKHA4_HUMAN] Epoxide hydrolase that catalyzes the final step in the biosynthesis of the proinflammatory mediator leukotriene B4. Has also aminopeptidase activity.<ref>PMID:1897988</ref> <ref>PMID:1975494</ref> <ref>PMID:2244921</ref> <ref>PMID:12207002</ref> <ref>PMID:11917124</ref> <ref>PMID:15078870</ref> <ref>PMID:18804029</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 23:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Hare~~, S A~~]]	+	[[Category: Hare SA]]
-	[[Category: Low~~, C M~~]]	+	[[Category: Low CM]]
-	[[Category: Snelgrove~~, R J~~]]	+	[[Category: Snelgrove RJ]]
-	[[Category: Wong~~, C T]]~~	+	[[Category: Wong CT]]
-	~~[[Category: Hydrolase]]~~	+
-	~~[[Category: Inflammation~~]]	+

OCA at 11:57, 26 August 2020

OCA — Wed, 26 Aug 2020 11:57:01 GMT

←Older revision		Revision as of 11:57, 26 August 2020
Line 1:		Line 1:

	==Crystal structure of LTA4H bound to a selective inhibitor against LTB4 generation==		==Crystal structure of LTA4H bound to a selective inhibitor against LTB4 generation==
-	<StructureSection load='5n3w' size='340' side='right' caption='[[5n3w]], [[Resolution\|resolution]] 2.30Å' scene=''>	+	<StructureSection load='5n3w' size='340' side='right'caption='[[5n3w]], [[Resolution\|resolution]] 2.30Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5n3w]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5N3W OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5N3W FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5n3w]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5N3W OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5N3W FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8KW:3-[2-(2-HYDROXYPHENYL)ETHYL]-5-METHOXY-PHENOL'>8KW</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8KW:3-[2-(2-HYDROXYPHENYL)ETHYL]-5-METHOXY-PHENOL'>8KW</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Leukotriene-A(4)_hydrolase Leukotriene-A(4) hydrolase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.3.2.6 3.3.2.6] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Leukotriene-A(4)_hydrolase Leukotriene-A(4) hydrolase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.3.2.6 3.3.2.6] </span></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5n3w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5n3w OCA], [http://pdbe.org/5n3w PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5n3w RCSB], [http://www.ebi.ac.uk/pdbsum/5n3w PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5n3w ProSAT]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5n3w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5n3w OCA], [http://pdbe.org/5n3w PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5n3w RCSB], [http://www.ebi.ac.uk/pdbsum/5n3w PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5n3w ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 23:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Hare, S A]]		[[Category: Hare, S A]]
	[[Category: Low, C M]]		[[Category: Low, C M]]

OCA at 13:47, 29 March 2017

OCA — Wed, 29 Mar 2017 13:47:46 GMT

←Older revision		Revision as of 13:47, 29 March 2017
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5n3w is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Crystal structure of LTA4H bound to a selective inhibitor against LTB4 generation==
		+	<StructureSection load='5n3w' size='340' side='right' caption='[[5n3w]], [[Resolution\|resolution]] 2.30Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5n3w]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5N3W OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5N3W FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8KW:3-[2-(2-HYDROXYPHENYL)ETHYL]-5-METHOXY-PHENOL'>8KW</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Leukotriene-A(4)_hydrolase Leukotriene-A(4) hydrolase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.3.2.6 3.3.2.6] </span></td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5n3w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5n3w OCA], [http://pdbe.org/5n3w PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5n3w RCSB], [http://www.ebi.ac.uk/pdbsum/5n3w PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5n3w ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/LKHA4_HUMAN LKHA4_HUMAN]] Epoxide hydrolase that catalyzes the final step in the biosynthesis of the proinflammatory mediator leukotriene B4. Has also aminopeptidase activity.<ref>PMID:1897988</ref> <ref>PMID:1975494</ref> <ref>PMID:2244921</ref> <ref>PMID:12207002</ref> <ref>PMID:11917124</ref> <ref>PMID:15078870</ref> <ref>PMID:18804029</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The pro-inflammatory mediator leukotriene B4 (LTB4) is implicated in the pathologies of an array of diseases and thus represents an attractive therapeutic target. The enzyme leukotriene A4 hydrolase (LTA4H) catalyses the distal step in LTB4 synthesis and hence inhibitors of this enzyme have been actively pursued. Despite potent LTA4H inhibitors entering clinical trials all have failed to show efficacy. We recently identified a secondary anti-inflammatory role for LTA4H in degrading the neutrophil chemoattractant Pro-Gly-Pro (PGP) and rationalized that the failure of conventional LTA4H inhibitors may be that they inadvertently prevented PGP degradation. We demonstrate that these inhibitors do indeed fail to discriminate between the dual activities of LTA4H, and enable PGP accumulation in mice. Accordingly, we have developed novel compounds that potently inhibit LTB4 generation whilst leaving PGP degradation unperturbed. These novel compounds could represent a safer and superior class of LTA4H inhibitors for translation into the clinic.

-	~~Authors: Wong, C.T~~., Low, ~~C.M.~~, ~~Snelgrove~~, ~~R.J.~~, Hare, S.A.	+	The development of novel LTA4H modulators to selectively target LTB4 generation.,Low CM, Akthar S, Patel DF, Loser S, Wong CT, Jackson PL, Blalock JE, Hare SA, Lloyd CM, Snelgrove RJ Sci Rep. 2017 Mar 17;7:44449. doi: 10.1038/srep44449. PMID:28303931<ref>PMID:28303931</ref>

-	~~Description: Crystal structure of LTA4H bound to~~ a ~~selective inhibitor against LTB4 generation~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
-	[[Category: Low, C.M]]	+	<div class="pdbe-citations 5n3w" style="background-color:#fffaf0;"></div>
-	[[Category: ~~Hare~~, ~~S.A~~]]	+	== References ==
-	[[Category: Wong, C.T]]	+	<references/>
-	[[Category: ~~Snelgrove, R.J~~]]	+	__TOC__
		+	</StructureSection>
		+	[[Category: Hare, S A]]
		+	[[Category: Low, C M]]
		+	[[Category: Snelgrove, R J]]
		+	[[Category: Wong, C T]]
		+	[[Category: Hydrolase]]
		+	[[Category: Inflammation]]

OCA: Protected "5n3w" [edit=sysop:move=sysop]

OCA — Thu, 09 Mar 2017 12:01:11 GMT

Protected "5n3w" [edit=sysop:move=sysop]

←Older revision

Revision as of 12:01, 9 March 2017

OCA: New page: '''Unreleased structure''' The entry 5n3w is ON HOLD until Paper Publication Authors: Wong, C.T., Low, C.M., Snelgrove, R.J., Hare, S.A. Description: Crystal structure of LTA4H bound t...

OCA — Thu, 09 Mar 2017 12:01:09 GMT

New page: '''Unreleased structure''' The entry 5n3w is ON HOLD until Paper Publication Authors: Wong, C.T., Low, C.M., Snelgrove, R.J., Hare, S.A. Description: Crystal structure of LTA4H bound t...

New page

'''Unreleased structure'''

The entry 5n3w is ON HOLD until Paper Publication

Authors: Wong, C.T., Low, C.M., Snelgrove, R.J., Hare, S.A.

Description: Crystal structure of LTA4H bound to a selective inhibitor against LTB4 generation
[[Category: Unreleased Structures]]
[[Category: Low, C.M]]
[[Category: Hare, S.A]]
[[Category: Wong, C.T]]
[[Category: Snelgrove, R.J]]