2y0j - Revision history

OCA at 10:43, 20 December 2023

OCA — Wed, 20 Dec 2023 10:43:10 GMT

←Older revision		Revision as of 10:43, 20 December 2023
Line 3:		Line 3:
	<StructureSection load='2y0j' size='340' side='right'caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>		<StructureSection load='2y0j' size='340' side='right'caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2y0j]] is a 2 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=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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]] 2.43Å</td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1lrb\|1lrb]], [[2wey\|2wey]]</div></td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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'>[https://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [https://pdbe.org/2y0j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [https://www.ebi.ac.uk/pdbsum/2y0j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2y0j 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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [https://pdbe.org/2y0j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [https://www.ebi.ac.uk/pdbsum/2y0j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2y0j ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN]] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.<ref>PMID:17389385</ref>	+	[https://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.<ref>PMID:17389385</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 27:		Line 26:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~3',5'-cyclic-nucleotide phosphodiesterase]]~~	+	[[Category: Homo sapiens]]
-	~~[[Category: Human~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Christoffersen~~, C T~~]]	+	[[Category: Christoffersen CT]]
-	[[Category: Kehler, J]]	+	[[Category: Kehler J]]
-	[[Category: Kilburn~~, J P~~]]	+	[[Category: Kilburn JP]]
-	[[Category: Langgard, M]]	+	[[Category: Langgard M]]
-	[[Category: Nielsen, J]]	+	[[Category: Nielsen J]]
-	[[Category: Petersen~~, S L~~]]	+	[[Category: Petersen SL]]
-	[[Category: Ritzen, A]]	+	[[Category: Ritzen A]]
-	~~[[Category: Hydrolase~~]]	+

OCA at 12:20, 27 April 2022

OCA — Wed, 27 Apr 2022 12:20:58 GMT

←Older revision		Revision as of 12:20, 27 April 2022
Line 3:		Line 3:
	<StructureSection load='2y0j' size='340' side='right'caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>		<StructureSection load='2y0j' size='340' side='right'caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lrb\|1lrb]], [[2wey\|2wey]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1lrb\|1lrb]], [[2wey\|2wey]]</div></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [~~http~~://pdbe.org/2y0j PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/2y0j PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=2y0j 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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [https://pdbe.org/2y0j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [https://www.ebi.ac.uk/pdbsum/2y0j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2y0j ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN]] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.<ref>PMID:17389385</ref>	+	[[https://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN]] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.<ref>PMID:17389385</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==

OCA at 12:29, 22 July 2020

OCA — Wed, 22 Jul 2020 12:29:17 GMT

←Older revision		Revision as of 12:29, 22 July 2020
Line 1:		Line 1:

	==Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors, part 2, Lead-optimisation.==		==Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors, part 2, Lead-optimisation.==
-	<StructureSection load='2y0j' size='340' side='right' caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>	+	<StructureSection load='2y0j' size='340' side='right'caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lrb\|1lrb]], [[2wey\|2wey]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lrb\|1lrb]], [[2wey\|2wey]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [http://pdbe.org/2y0j PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [http://www.ebi.ac.uk/pdbsum/2y0j PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2y0j 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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [http://pdbe.org/2y0j PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [http://www.ebi.ac.uk/pdbsum/2y0j PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2y0j ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 22:		Line 22:

	==See Also==		==See Also==
-	*[[Phosphodiesterase\|Phosphodiesterase]]	+	*[[Phosphodiesterase 3D structures\|Phosphodiesterase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 29:		Line 29:
	[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]		[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Christoffersen, C T]]		[[Category: Christoffersen, C T]]
	[[Category: Kehler, J]]		[[Category: Kehler, J]]

OCA at 09:00, 10 October 2018

OCA — Wed, 10 Oct 2018 09:00:45 GMT

←Older revision		Revision as of 09:00, 10 October 2018
Line 1:		Line 1:

-	==~~TRIAZOLOQUINAZOLINES AS A NOVEL CLASS OF PHOSPHODIESTERASE~~ 10A (PDE10A) ~~INHIBITORS~~, ~~PART~~ 2, ~~LEAD~~-~~OPTIMISATION~~.==	+	==Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors, part 2, Lead-optimisation.==
	<StructureSection load='2y0j' size='340' side='right' caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>		<StructureSection load='2y0j' size='340' side='right' caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>
	== Structural highlights ==		== Structural highlights ==

OCA at 05:33, 5 August 2016

OCA — Fri, 05 Aug 2016 05:33:34 GMT

←Older revision		Revision as of 05:33, 5 August 2016
Line 1:		Line 1:
		+
	==TRIAZOLOQUINAZOLINES AS A NOVEL CLASS OF PHOSPHODIESTERASE 10A (PDE10A) INHIBITORS, PART 2, LEAD-OPTIMISATION.==		==TRIAZOLOQUINAZOLINES AS A NOVEL CLASS OF PHOSPHODIESTERASE 10A (PDE10A) INHIBITORS, PART 2, LEAD-OPTIMISATION.==
	<StructureSection load='2y0j' size='340' side='right' caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>		<StructureSection load='2y0j' size='340' side='right' caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with 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=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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"><scene name='pdbligand=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lrb\|1lrb]], [[2wey\|2wey]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lrb\|1lrb]], [[2wey\|2wey]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [http://www.ebi.ac.uk/pdbsum/2y0j PDBsum]</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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [http://pdbe.org/2y0j PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [http://www.ebi.ac.uk/pdbsum/2y0j PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2y0j ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 18:		Line 19:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 2y0j" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 26:		Line 28:
	</StructureSection>		</StructureSection>
	[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]		[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Christoffersen, C T]]		[[Category: Christoffersen, C T]]
	[[Category: Kehler, J]]		[[Category: Kehler, J]]

OCA at 23:25, 24 December 2014

OCA — Wed, 24 Dec 2014 23:25:15 GMT

←Older revision		Revision as of 23:25, 24 December 2014
Line 8:		Line 8:
	<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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [http://www.ebi.ac.uk/pdbsum/2y0j PDBsum]</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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [http://www.ebi.ac.uk/pdbsum/2y0j PDBsum]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN]] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.<ref>PMID:17389385</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 25:		Line 27:
	[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]		[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Christoffersen, C T.]]	+	[[Category: Christoffersen, C T]]
-	[[Category: Kehler, J.]]	+	[[Category: Kehler, J]]
-	[[Category: Kilburn, J P.]]	+	[[Category: Kilburn, J P]]
-	[[Category: Langgard, M.]]	+	[[Category: Langgard, M]]
-	[[Category: Nielsen, J.]]	+	[[Category: Nielsen, J]]
-	[[Category: Petersen, S L.]]	+	[[Category: Petersen, S L]]
-	[[Category: Ritzen, A.]]	+	[[Category: Ritzen, A]]
	[[Category: Hydrolase]]		[[Category: Hydrolase]]

OCA at 13:09, 22 October 2014

OCA — Wed, 22 Oct 2014 13:09:06 GMT

←Older revision		Revision as of 13:09, 22 October 2014
Line 1:		Line 1:
-	[[~~Image:~~2y0j.~~png~~\|~~left~~\|~~200px~~]]	+	==TRIAZOLOQUINAZOLINES AS A NOVEL CLASS OF PHOSPHODIESTERASE 10A (PDE10A) INHIBITORS, PART 2, LEAD-OPTIMISATION.==
		+	<StructureSection load='2y0j' size='340' side='right' caption='[[2y0j]], [[Resolution\|resolution]] 2.43Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[2y0j]] is a 2 chain structure with 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=2Y0J OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2Y0J FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AXC:5-(1H-BENZIMIDAZOL-2-YLMETHYLSULFANYL)-2-METHYL-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLINE'>AXC</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lrb\|1lrb]], [[2wey\|2wey]]</td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/3',5'-cyclic-nucleotide_phosphodiesterase 3',5'-cyclic-nucleotide phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.17 3.1.4.17] </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=2y0j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y0j OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2y0j RCSB], [http://www.ebi.ac.uk/pdbsum/2y0j PDBsum]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Novel triazoloquinazolines have been found as phosphodiesterase 10A (PDE10A) inhibitors. Structure-activity studies improved the initial micromolar potency which was found in the lead compound by a 100-fold identifying 5-(1H-benzoimidazol-2-ylmethylsulfanyl)-2-methyl-[1,2,4]triazolo[1,5-c]qui nazoline, 42 (PDE10A IC(50)=12nM) as the most potent compound from the series. Two X-ray structures revealed novel binding modes to the catalytic site of the PDE10A enzyme.

-	~~{{STRUCTURE_2y0j\| PDB=2y0j \| SCENE= }}~~	+	Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.,Kehler J, Ritzen A, Langgard M, Petersen SL, Farah MM, Bundgaard C, Christoffersen CT, Nielsen J, Kilburn JP Bioorg Med Chem Lett. 2011 Jun 15;21(12):3738-42. Epub 2011 Apr 30. PMID:21602043<ref>PMID:21602043</ref>

-	~~===TRIAZOLOQUINAZOLINES AS A NOVEL CLASS OF PHOSPHODIESTERASE 10A (PDE10A) INHIBITORS~~, ~~PART 2, LEAD-OPTIMISATION.===~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~{{ABSTRACT_PUBMED_21602043}}~~	+
-		+
-	~~==About this Structure==~~	+
-	~~[[2y0j]] is~~ a ~~2 chain structure with 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=2Y0J OCA].~~	+

	==See Also==		==See Also==
	*[[Phosphodiesterase\|Phosphodiesterase]]		*[[Phosphodiesterase\|Phosphodiesterase]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	<~~ref group="xtra">PMID:021602043<~~/~~ref~~><~~references group="xtra"~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]		[[Category: 3',5'-cyclic-nucleotide phosphodiesterase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]

OCA at 10:11, 20 October 2012

OCA — Sat, 20 Oct 2012 10:11:09 GMT

←Older revision		Revision as of 10:11, 20 October 2012
Line 8:		Line 8:

	==About this Structure==		==About this Structure==
-	[[2y0j]] is a 2 chain structure ~~of [[Phosphodiesterase]]~~ with 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=2Y0J OCA].	+	[[2y0j]] is a 2 chain structure with 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=2Y0J OCA].

	==See Also==		==See Also==

OCA at 01:16, 26 July 2012

OCA — Thu, 26 Jul 2012 01:16:21 GMT

←Older revision		Revision as of 01:16, 26 July 2012
Line 1:		Line 1:
-	[[Image:2y0j.~~jpg~~\|left\|200px]]	+	[[Image:2y0j.png\|left\|200px]]

-	<!--
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	{{STRUCTURE_2y0j\| PDB=2y0j \| SCENE= }}		{{STRUCTURE_2y0j\| PDB=2y0j \| SCENE= }}

	===TRIAZOLOQUINAZOLINES AS A NOVEL CLASS OF PHOSPHODIESTERASE 10A (PDE10A) INHIBITORS, PART 2, LEAD-OPTIMISATION.===		===TRIAZOLOQUINAZOLINES AS A NOVEL CLASS OF PHOSPHODIESTERASE 10A (PDE10A) INHIBITORS, PART 2, LEAD-OPTIMISATION.===

-
-	<!--
-	The line below this paragraph, {{ABSTRACT_PUBMED_21602043}}, adds the Publication Abstract to the page
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	{{ABSTRACT_PUBMED_21602043}}		{{ABSTRACT_PUBMED_21602043}}

	==About this Structure==		==About this Structure==
-	[[2y0j]] is a 2 chain structure with 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=2Y0J OCA].	+	[[2y0j]] is a 2 chain structure of [[Phosphodiesterase]] with 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=2Y0J OCA].
		+
		+	==See Also==
		+	*[[Phosphodiesterase\|Phosphodiesterase]]

	==Reference==		==Reference==

OCA: Protected "2y0j" [edit=sysop:move=sysop]

OCA — Wed, 15 Jun 2011 06:21:52 GMT

Protected "2y0j" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:21, 15 June 2011